-------------------------------------------------------------------------------
      Synthesis of  the Fentanyl analog beta-hydroxy-alpha-methylfentanyl
-------------------------------------------------------------------------------

First a quick summary:
----------------------

Rev drone:

Alright, I'm only gonna say this once...

N-methyl-4-piperidone + methyl iodide  ===>
N,N-dimethyl-4-piperidone iodide + phenylpropanolamine, base ===>
beta-hydroxy-alpha-methyl-phenylethyl-4-piperidone + aniline, NaBH4 ===>
4-anilo-1-(beta-hydroxy-alpha-methyl-phenethyl)-piperidone + (CH3CH2CO)2O ===>
beta-hydroxy-alpha-methylfentanyl

Next, you'll want ref's, I bet. Ho-hum. Invariably, Step 2 (the replacement
of the quaternary amine with phenylpropanolamine) is the one you're wondering
about, isn't it? I thought so.

        Chem.Heterocycl.Compd.; 21; 12; 1985; 1355-1362;

You probobly want to know a little about reductive
amination of aniline with your piperidone, too.

        Chem.Pharm.Bull.; 33; 5; 1985; 1826-1835;

Just to be thorough, here's the addition of the propionyl group:

        J.Heterocycl.Chem.; 26; 1989; 677-686;

The reasons for doing this are numerous. N-methyl piperidone is unwatched,
available in big quantities, and very cheap.

-------------------------------------------------------------------------------
The Hive BB - Chemistry Discourse

Topic: a gift from drone to the DEA -- a little china white

Drone 342:
 Get ready for some gut-pumpin' chemical fun!

 As a gift from my workin' class worker bee
 subconscious to you, the larger community, here's a
 little genie that I've been struggling to keep in the
 bottle now for a year. "Pop", goes the cork, and like
 a little butterfly, this chemical nugget spreads its
 wings for the rest of the word.

 Drone's home-made fentanyl analog!

 Yep, drone has doen what was thought impossible, and
 will now divulge what is thought unmentionable,
 because DRONE #342 is DRONE #342, and can do that!

 Folks, have you ever had a hankering for a big, juicy
 ounce or two of synthetic heroin, but just thought it
 impossible to allocate the necessary chemicals? Well,
 your friend drone has taken out the guesswork and
 managed to develope a synthetic route to a chemical
 1000 or so stronger than conventional smack.
 Impossible, you say? NAY, my dear worker bees.

 Here's the general overview of fentanyl synthesis.
 4-piperidone is reacted with a trimethyliodo
 (quaternary) salt of a phenethylamine (or any number
 of aromatic ethylamines), to produce an
 N-arylethylpiperidone (you can use the quaternary salt
 of the piperidone with the primary substituted
 arylethytlamine, if you like, too.) Anyways, this is
 reacted with aniline, and reduced with NaBH4, and then
 reacted with propionic anhydride to produce the
 fentanyl freebase.

 It turns out:

 *adding an ethyl carbon bridge to the piperidine ring
 will not reduce potency.

 *adding an extra methyl to the phenethyl substituent
 to make a phenylisopropyl makes for a strong,
 long-lasting compound.

 *adding a hydroxy to the alpha-carbon of the pehethyl
 side chain -- as seen in ephedrine -- will also
 increase potency.

 *as I said in a previous post, propionic anhydride can
 be made at home (this is the most closely watched
 chemical on the DEA's list, but this watching was
 rendered obsolete by YoursTruly not too long ago.)

 The Fentanyl Suite, in d(l)-major; Movement 1

 (the curtain rises, our anti-hero is found quietly
 sauntering through the woods, foraging for
 precursors.)

 Taking this into account, Atropine is extracted from
 nightshade. It is hydrolyzed to form tropine. Tropine
 is oxidized to form tropinone. Tropinone is then
 exhaustively methylated with iodomethane.

 Second Movement

 Dexatrim is bought in a fiendish quantity. The PPA is
 extracted and isolated as its free base. This is
 combined with tropinone, to form
 N-(1-hydroxy-1-phenyl)isopropyl tropinone.

 (intermezzeo)

 Third Movement

 Aniline is combined with the aforementioned
 freshly-made tropinone, and reduced with NaBH4.

 Fourth Movement
 (Allegro)

 Propionic anhydride is made from a propionate salt
 like calcium propionate by adding bromine or even
 chlorine. Alternatively, propionate esters are
 hydrolyzed, the acid component isolated, and combined
 with acetic anhydride and allowed to reflux, with the
 product being fractionally distilled.

 (crescendo)

 The propionic anhydride is added to our soon-to-be
 fentanyl analog compound, and allowed to react (I
 think around 50 C). The product is flash
 chromatographed, combined with citric acid (or any
 acid of your choice), and allowed to dry.

 The material is cut with hundreds of times its mass of
 mannitol.

 Viola! China white has just been made out of
 Nightshade, diet tablets, aniline, and food
 preservatives. It's all there in the literature. Ref's
 available upon request.

 Are we having fun yet?

 -drone #342

-------------------------------------------------------------------------------
Rhodium (Administrator)

Could we have a little more pharmacological data on this compound?

I'd like to have the ref on reacting a quat with 4-piperidone, to give the
tertiary amine. If you have any refs on making 4-piperidone, that would be nice
too.

Tropinone is easily made from citric acid, methylamine and succinic dialdehyde
(made from pyrrole). You can also make cocaine from it :)

-------------------------------------------------------------------------------
drone 3422 - posted 05-19-98 08:50 PM

   -------------------------------------------------------

The Robinson tropine synthesis isn't all its cracked up to be -- the main
detraction is that succinaldehyde. Have you ever looked at its synthesis? At
least the means that I found didn't look too appetizing; I'd extract tropines
and hydrolyze and oxidize them over that any day of the week.

I'll get you the ref's on this tommorow.

-------------------------------------------------------------------------------

Rhodium

Yes, I've looked into the synthesis. Even going the whole way to cocaine isn't
that hard in my opinion. But back to tropinone. I'd very much rather make it
myself, than poison myself with atropine alkaloids.

Succindialdehyde is made from pyrrole by refluxing with hydroxylamine and KOH.


Solomon

Hey drone, thanks alot for this great stuff.

                                      Have you ever heard of PePAP (The meperidine anolog)?
                                      It's (1-(2-Phenylethyl)-4-acetyloxpiperidine) I think.
                                      Sounds kind of interesting to me.

   drone 342                          [Image] posted 05-20-98 09:43 AM
   Member
                                      [Click Here to See the Profile for drone 342]
                                      -------------------------------------------------------
                                      Here's a ref or two.

                   For the addition elimination with the quat amine,
                   check out:
                   Chem. Het. Comp. 21:2, (1985) 1355-1362

                   There's another one somewhere around in my piles of
                   shit, butI can't find it. This one is good though, and
                   should help you out quiite nicely.

                   For piperidone synths:
                   JACS 53 1931 2693, 2696
                   Helv. Chim. Acta 3, 1920, 815
                   JOC 37 1972 1042-1045
                   JCS 1952, 1164, 1167
                   Yakugaku Zasshi 71 1951 1053, 1056
                   JOC 10, 1945, 277, 279
                   JCS 1949, 708, 711
                   JACS 70, 1948 1820,1822

                   for tropinone-based fentanyls' chemistry and/or
                   pharmacology:
                   JMC 22, 1167 (1979)
                   J. Het. Chem. 14, 599 (1977)
                   Org. Magn. Reson. 6, 441 (1974)

                   For carfentanyl:
                   DE PAT 2610228, 1976
                   US PAT 4179569, 1979
                   Arzneim Forsch 26, 1976 1521, 1523, 1528

                   There, that ought keep ya busy!

                   -drone #342

   drone 342       [Image] posted 05-20-98 06:19 PM
   Member
                   [Click Here to See the Profile for drone 342]
                   -------------------------------------------------------
                   Rhodium,

                   Tropninonecan be hydrolyzed from atropine in
                   nightshade quite easily. A little acid-base
                   extraction, followed by vacuum distillation, will give
                   you an excellent product for xoidizing into tropinone.
                   Its cheap and plentiful. On top of that, its
                   uncontrollable and essentially unlimited.

                   However, if you do come across some really facile way
                   of making that succinaldehyde and feel like posting
                   it, I have some excellent ref's for some wacky
                   benztropine analogs that put coke itself to shame
                   (judging by the pharmacology reports and biological
                   assays, these little goodies will pump-n-suck your
                   dopamine receptors like you know how you want them
                   to.)

                   -drone #342

   drone 342       [Image] posted 05-20-98 08:12 PM
   Member
                   [Click Here to See the Profile for drone 342]
                   -------------------------------------------------------
                   Here's some stuff from Beilstein on thebaine
                   isolation. I actually have more at home than this, but
                   I just couldn't get it all together this morning.
                   Anyways, here you go:

                   Isolation From Natural Product Isolierung aus Opium
                   Ref. 1 761186; Patent; Knoll A.G.; US 2712018; 1951;
                   Ref. 2 761187; Journal; Heumann; BNUNA5; Bull.Narc.;
                   9; 2; 1957; 34;
                   -------------------------

                   Isolation From Natural Product 2 of 13
                   Isolation From Natural Product Bldg. in Samen u.
                   Keimlingen von Papaver bracteatum
                   Ref. 1 3022808; Journal; Sarkany et al.; PLMEAA;
                   Planta Med.; 36; 1979; 289;
                   -------------------------

                   Isolation From Natural Product 3 of 13 Isolation From
                   Natural Product Papaver albiflorum PACZ. subsp.
                   albiflorum
                   Ref. 1 5559025; Journal; Slavik, Jiri; Slavikova,
                   Leonora; Dolejs, Ladislav; CCCCAK;
                   Collect.Czech.Chem.Commun.; EN; 46; 10; 1981;
                   2587-2593;
                   -------------------------

                   Isolation From Natural Product 4 of 13
                   Isolation From Natural Product Papaver bracteatum
                   Ref. 1 3022810; Journal; Levy et al.; PLMEAA; Planta
                   Med.; 36; 1979; 362,364;
                   -------------------------

                   Isolation From Natural Product 5 of 13
                   Isolation From Natural Product Papaver bracteatum
                   LINDL.
                   Ref. 1 5557634; Journal; Slavik, Jiri; Slavikova,
                   Leonora; CCCCAK; Collect.Czech.Chem.Commun.; EN; 50;
                   5; 1985; 1216-1226;
                   -------------------------

                   Isolation From Natural Product 6 of 13
                   Isolation From Natural Product Papaver bracteatum Arya
                   II
                   Ref. 1 5910497; Journal; Meshulam, Haim; Lavie, David;
                   PYTCAS; Phytochemistry; EN; 19; 1980; 2633-2636;
                   -------------------------

                   Isolation From Natural Product 7 of 13
                   Isolation From Natural Product Papaver fugax
                   Ref. 1 3017192; Journal; Sariyar et al.; PYTCAS;
                   Phytochemistry; 12; 1973; 2431,2433;
                   -------------------------

                   Isolation From Natural Product 8 of 13
                   Isolation From Natural Product Papaver oreophilum
                   Ref. 1 3022809; Journal; Maturova et al.; PLMEAA;
                   Planta Med.; 14; 1966; 22,38;
                   -------------------------

                   Isolation From Natural Product 9 of 13
                   Isolation From Natural Product Papaver setigerum DC.
                   Ref. 1 6038149; Journal; Slavik, Jiri; Slavikova,
                   Leonora; CCCCAK; Collect.Czech.Chem.Commun.; EN; 61;
                   7; 1996; 1047-1052;
                   -------------------------

                   Isolation From Natural Product 10 of 13
                   Isolation From Natural Product Papaver somniferum
                   Ref. 1 64358; Journal; Parker,H.I. et al.; JACSAT;
                   J.Amer.Chem.Soc.; EN; 94; 1972; 1276-1282;
                   -------------------------

                   Isolation From Natural Product 11 of 13
                   Isolation From Natural Product Papaver somniferum
                   Ref. 1 163865; Journal; Barton,D.H.R. et al.; JCSOA9;
                   J.Chem.Soc.; EN; 1965; 2423-2438;
                   -------------------------

                   Isolation From Natural Product 12 of 13
                   Isolation From Natural Product Papaver somniferum
                   Ref. 1 5829983; Journal; Waddell, Thomas G.; Rapoport,
                   Henry; PYTCAS; Phytochemistry; EN; 24; 3; 1985;
                   469-472;
                   -------------------------

                   Isolation From Natural Product 13 of 13
                   Isolation From Natural Product Papaver somniferum
                   after extraction with aqueous sodium bisulphite,
                   removing morphine and codeine and extraction with
                   acetic acid
                   Ref. 1 5856249; Journal; Repasi, Janos; Hosztafi,
                   Sandor; Szabo, Zoltan; PLMEAA; Planta Med.; EN; 59; 5;
                   1993; 477-478;

   drone 342       [Image] posted 05-20-98 08:33 PM
   Member
                   [Click Here to See the Profile for drone 342]
                   -------------------------------------------------------
                   Sorry about that; this last message belongs in the
                   current opium thread in the novel discussion area.

                   imagine my chagrin,

                   -drone #342

   Rhodium         [Image] posted 05-24-98 08:19 PM
   Administrator
                   [Click Here to See the Profile for Rhodium]
                   -------------------------------------------------------

                   Succinaldehyde [JACS 68, 1608-1610 (1946)]

                   Various procedures, usually applicable for the
                   preparation of aldehydes from appropriate
                   intermediates, were tried unsuccessfully: e. g., the
                   distillation of mixed calcium succinate and calcium
                   formates, a Rosenmund type of reduction of succinyl
                   chloride, the partial hydrogenation of succinonitrile,
                   either catalytically or by Stephen's methods with
                   stannous chloride, to the diimine; all gave no trace
                   of the desired aldehyde. Bromo- and chloroacetal do
                   not undergo the Fittig condensation, but instead yield
                   ethyl vinyl ether. The Grignard condensation of
                   beta-halogenopropionaldehyde acetal with ethyl
                   orthoformate, expected to yield the tetraethyl acetal
                   of succinaldehyde, was not tried since neither
                   beta-chloro- nor beta-bromopropionaldehyde acetal
                   would react with magnesium. Hence, resort was made to
                   the synthesis of succinaldehyde from pyrrole, via the
                   dioxime, and a procedure was employed which does not
                   require the isolation of the dialdehyde.

                   Succinaldoxime
                   In a 2-liter, 3-necked flask, equipped with mechanical
                   stirrer and reflux condenser, were placed 1 liter of
                   ethanol, 67 g freshly distilled pyrrole, and 141g
                   hydroxylamine hydrochloride. The mixture was stirred
                   and heated to refluxing, as soon as solution was
                   complete 106g anhydrous sodium carbonate was added, in
                   small portions, as rapidly as possible; and the
                   solution was then refluxed for-twenty-four hours. The
                   hot alcoholic mixture was then filtered to remove
                   sodium chloride, and the filtrate was evaporated to
                   dryness under reduced pressure. The residue was taken
                   up in the minimum of boiling water, the solution
                   heated with decolorizing charcoal, filtered and the
                   product allowed to crystallize in the refrigerator.
                   Additional product could be obtained by concentrating
                   the mother liquors. The yield of dioxime varied from
                   40 to 44g, 35 to 38%, and the product melted at
                   171-172¡C.

                   Succinaldehyde
                   A twentieth mole, 5.8g, of succinaldoxime was placed
                   in a beaker of 250 ml. capacity and 54 ml. of 10%
                   sulfuric acid was added. The mixture was cooled to 0¡C
                   and to it was added, in small portions, 7.0g of sodium
                   nitrite, keeping the temperature at 0¡C. Evolution of
                   nitrogen dioxide fumes indicates too rapid addition of
                   the nitrite. The dioxime was now completely dissolved,
                   and the solution was allowed to warm
                   slowly to 20¡C and effervescence to go to completion.
                   The lemon-colored solution was then neutralized to
                   litmus by the addition of small portions of barium
                   carbonate, and the precipitated barium sulfate was
                   removed, leaving the free succinaldehyde in the
                   filtrate. The solution was assayed at this point by
                   precipitating quantitatively from an aliquot portion
                   the bis-2,4-dinitrophenylhydrazone; the weight of
                   crude derivative showed that consistent yields of 90%
                   of the dialdehyde could be expected. Since this
                   solution was found satisfactory for these studies, the
                   aldehyde was not isolated, thus avoiding loss of
                   product. The bis-dinitrophenylhydrazone, after
                   recrystallization from alcohol, melted at 278-280¡C.

                   Succindialdoxime [JOC 21, 644-647 (1956)]

                   Hydroxylamine hydrochloride (90.5 g., 1.30 moles) was
                   pulverized and stirred 30 minutes at room temperature
                   with alcohol (400 ml). A solution of potassium
                   hydroxide (44.8 g, 0.8 mole) in water (50 ml.) and
                   alcohol (50 ml) was added. To the thick mixture
                   pyrrole (34.5 ml, 0.5 mole) was admitted and the whole
                   was refluxed gently for 23 hours, during which period
                   it gradually turned orange-brown
                   and gave off ammonia. Alcohol (100 ml) was added,
                   refluxing continued another hour, and the mixture was
                   filtered hot with suction. The inorganic residue was
                   washed white with hot alcohol (100 ml), and the dark
                   filtrate and washings were concentrated under vacuum
                   to a tan semi-solid which was collected and washed
                   with a little alcohol: 56 g. When treated with 18 N
                   sulfuric acid, the vacuum distillate turned
                   bluish-green and deposited hydroxylamine hydrosulfate
                   (1.8 g). The filtrate and washings, which had an odor
                   reminiscent of indole, containedtarry impurities and
                   hydroxylamine hemichloride (~8 g). The tan residue (56
                   g) was mixed with an equal weight of water
                   (endothermicity!) and, after a half hour, the
                   water-soluble impurities (ammonium chloride and
                   hydroxylamine hemichloride) were filtered off leaving
                   35.5g (61%); This product ras recrystallized by
                   addition of six times its weight of boiling water,
                   swirling occasionally until dissolved, adding Darco
                   (4g), and filtering after 2 minutes through Super-Cel
                   with suction. The yellow filtrate soon deposited
                   crystals and, after storing 2 days at 5¡C, the
                   succindialdoxime was collected; 30.4 grams (52%) of
                   pale yellow crystals, mp 169-170¡C.

   Osmium          [Image] posted 05-26-98 04:58 AM
   Member
                   [Click Here to See the Profile for Osmium]
                   -------------------------------------------------------
                   Give us your coke analogue refs, drone.
                   Please.

   Piglet          [Image] posted 05-26-98 10:14 AM
   Member
                   [Click Here to See the Profile for Piglet]
                   -------------------------------------------------------
                   While we are on the subject of potent analogues, can
                   anyone comment on the cocaine analogue with a P-Fluoro
                   group on the benzoic acid ? the Future Synthetic Drugs
                   of Abuse says that it is 60 times stronger than the
                   parent compound. Many moons ago I suggested that this
                   could be made by purchacing cocaine, purifying it and
                   converting it to ecgonine using CaO and then reacting
                   it with HCl/Methanol to get the methyl ester & then
                   Para Fluoro Benzoic Acid. The PFBA could be made from
                   Para Amino Benzoic Acid (health food shop!) via NaNO2
                   to produce the diazonium salt and then reaction with
                   sodium fluoroborate or fluoroboric acid (careful!).
                   Fluoroboric acid can be made from hydrofluoric acid &
                   boric acid. You can't use glass for this bit & the
                   fluoride WILL send you to an early grave if you make a
                   mistake.
                   Ammonium flouride can be purchased to clean concrete
                   off glass & for glass etching.

   drone 342       [Image] posted 05-26-98 10:49 AM
   Member
                   [Click Here to See the Profile for drone 342]
                   -------------------------------------------------------
                   for benztropine analogs that are fun:

                   US Pat 2799680 (1954)
                   US Pat 2706198 (1952)
                   JMC 37, 15, (1994 2258-2261
                   JMC 38, 20, (1995)3933-3940

                   for CIT and other coke-esque analogs:
                   JMC 34, 10, (1991) 2719-2725
                   JMC 34, 10, (1991) 3144-3146
                   JMC 35, 13, (1992) 2497-2500
                   JMC 35, 25, (1992) 4764-4766
                   JMC 36, 7, (1993) 855- 862
                   JMC 36, 20, (1993) 2886-2890
                   JMC 37, 8, (1994) 1220-1223
                   JMC 37, 10, (1994) 1535-1542
                   JMC 37, 11, (1994) 1558-1561
                   JMC 37, 18, (1994) 2865-2873
                   JMC 38, 2, (1995) 379- 388
                   JMC 38, 16, (1995) 3086-3093

                   This is an incomplete list; I have a stack of xeroxes
                   of articles realted to these chemicals that's about 3
                   inches thick. Turns out, if you wire the phenyl group
                   directyly to the tropane ring (no oxygens or
                   carbonyls, or whatever), potency increases. In
                   addition, it apprears the general rule is that
                   substituents on the 4-position of the phenyl generally
                   increase potency. As for benztropine, it turns out
                   that if you add halides on its phenyl groups at the
                   4-position, you get something much more selective for
                   dopamine, and much less of an anticholinergic, which
                   translates to a better (higher) ratio of
                   tweak:wierdness than coke.

                   This is one of my last posts for a long time, so I
                   hope this helps out. Keep up the good fight.

                   -drone #342

   336669          [Image] posted 07-20-98 05:09 PM
   Member
                   [Click Here to See the Profile for 336669]
                   -------------------------------------------------------
                   wow! you guys really know your stuff, huh? I'm
                   impressed!

   drone 342       [Image] posted 07-21-98 11:03 AM
   Member
                   [Click Here to See the Profile for drone 342]
                   -------------------------------------------------------
                   Piglet, here are actually analogs of that cocain
                   derivative that are even STRONGER. I'm awat from my
                   ref's, but if you look up that fluorophenylecgognine
                   analog using Beilstein, it'll list many more articles
                   covering them.

                   -drone #342

   drone 342       [Image] posted 07-21-98 11:06 AM
   Member
                   [Click Here to See the Profile for drone 342]
                   -------------------------------------------------------
                   336669, thanks. I'm glad our work is appreciated. I've
                   always felt that fentanyls could act as sort of the
                   heavy artillary of the WOD's. Considering thier dosage
                   size, and the materials they can be made out of
                   they're unstoppable (look what a problem speed is, now
                   imagine a drug with a dosage *SEVERAL ORDERS OF
                   MAGNITUDE SMALLER*!)

   BOZAKIUM        [Image] posted 07-21-98 04:27 PM
                   [Click Here to See the Profile for BOZAKIUM]
                   -------------------------------------------------------
                   shit! this thread made me bust a nut in my pants!!! I
                   have always wanted a good lead on the fentanyls, and
                   y'all bees have opened the door for me. Thanx. For the
                   money people out there, a pound of methyl fentanyl is
                   worth over a bilion dollars. It would be great for
                   someone to do a PIHKAL-type project on all the
                   fentanyls AND coke analogues.mmm-mmm.

   The Alchemist   [Image] posted 07-22-98 08:25 PM
   Member
                   [Click Here to See the Profile for The Alchemist]
                   -------------------------------------------------------
                   I would love to dream up some methyl-fetanyl but
                   there's always that old story of the MPTP byproduct.
                   Under what conditions is this byproduct made and
                   what's the best way to keep it out?

                   Clueless on the fentanyl scene but mmmmmmm... does it
                   sound yummy.

                   -the alchemist

   drone 342       [Image] posted 07-24-98 09:37 AM
   Member
                   [Click Here to See the Profile for drone 342]
                   -------------------------------------------------------
                   Boz,

                   A HardDrug-iHKAL-thingy is already in the works!

                   MTPT is not a byproduct from fentanyls, but rather
                   from some extremely potent pethidine analogs. Both
                   opioid agonists, but I never understood why one would
                   rather make pethidine over fentanyl. It was the result
                   of high temps and/or low pH's at a particular step,
                   but don't quote me on that.

                   The most important thing here hygene. This stuff is
                   extremely potent, and the last thing you want to do is
                   accidentally breath in a milligram while working with
                   it.

                   -drone #342

   Osiris          [Image] posted 07-25-98 04:13 PM
   Junior Member
                   [Click Here to See the Profile for Osiris]
                   -------------------------------------------------------
                   Drone, these fentanyls sound very interesting.
                   Unfortunately, I do not see them taking over the
                   world, due to the fact that they are so powerful. In
                   the LSD world, the chemist can produce liquid and just
                   pass it down to the people farther down the chain for
                   them to cut and/or soak into blotter paper. I am
                   assuming that the entanyls would be primarily
                   distributed via blotter also. If one of the
                   distributors fucks up and accidentally makes blotter
                   without cutting and each blotter has 1 mg LSD, the
                   unwitting ingestors will trip very hard but since it
                   is impossible to OD on LSD with anything anywhere
                   close to a normal dose, they will still be physically
                   safe.

                   Make a similar mistake with fentanyls, though, and
                   people will be dropping like flies, right? That sort
                   of thing tends to put people off your product. To
                   avoid this possibility, the chemist will have to make
                   up the blotters himself. If the chemist makes up ten
                   million doses of his fentanyl, that means that he has
                   to dip one hundred thousand blotter cards himself.
                   Even if our chemist can come up with a way to do this
                   more quickly and easily, he still has to figure out a
                   way to purchase 100,000 blotter cards without drawing
                   a lot of heat. And then he has to figure out how to
                   MOVE all of that bulky paper.

                   I have never been involved with anything of this
                   nature, so this is all speculation and I might be
                   wrong. If so, please correct me. It would be cool if
                   massive fentanyl manufacturing, packaging and
                   distribution could be made to work well - if nothing
                   else, it would keep a lot of addicts from having to
                   stick needles in themselves many times a day to get
                   their fix, which would be a huge boon to overall
                   public health.

   bootie rocket   [Image] posted 07-25-98 05:54 PM
                   [Click Here to See the Profile for bootie rocket]
                   -------------------------------------------------------
                   Perhaps it could be dissolved in a solvent and sprayed
                   on an inactive powder and snorted. I'm not into H or
                   it's derivitives but I can think of the way most H
                   masters I've seen prefer to do it, and it aint
                   snorting;)
                   You sick little monkeys, I love ya! -BR

   ICEKAT          [Image] posted 07-26-98 05:00 PM
   Member
                   [Click Here to See the Profile for ICEKAT]
                   -------------------------------------------------------
                   Hello ALL,

                   I participated in a study at the univestity s
                   departmant of anesthesiology with fentanyl and let me
                   tell you it is a potentially very very dangerous drug.
                   I say that because I know first hand. It has some some
                   terrible side affects like at high doses riggitity and
                   contraction of muscles, plus a not to unpleasant
                   itchie eyes, nose, and back. You feel great at first
                   but I at a very high dose decided I didn't need to
                   breath. I was so out of it the staff had to shake me
                   and tell me to remember to breath. I would then
                   remember and breath but soon forget again until I
                   became completly unresponsive and had to be resperated
                   and brought down. I did this two times. And was
                   artificialy resperated both times. The nausia is
                   terrible, and Dry heaved twice even though I had
                   fasted and no liquids and I felt terrilble. This drug
                   is for only the most responcible of types because
                   dosage is very very very very very critical. I was
                   lucky enough to get the experience in a very controled
                   stetting with a group of trained profesionals working
                   to make sure everything would be ok. A little oops and
                   say goodbye cause your going to forget to breath. I
                   would suggest selling Naloxone (SP?) with any and all
                   that gets on the streat because that is one of the
                   only drugs to bring you down in case of overdose. Or a
                   automatic resperator would work well to.

                   BECAREFUl!!!!!!!!!!!!!!!!!!!!

                   ICEKAT

   drone 342       [Image] posted 07-26-98 06:19 PM
   Member
                   [Click Here to See the Profile for drone 342]
                   -------------------------------------------------------
                   Osiris,

                   I see what you mean, but this is not the case.
                   Fentanyl would obviously be mixed with something like
                   mannitol to dlute it to a more manageable size.

                   Why would anybody want to do blotter smack?

                   In any case, you're worried about some dealer fucking
                   up with measurements -- which is a reasonable concern.
                   However, with fentanyls, its actaully SAFER than other
                   comparable drugs. The therapeutic index for fentanyls
                   is much higher than for heroin, so that you actually
                   have a safer product. There's a wider safety margin
                   with fentanyls than with opiates or any other opioids
                   -- making this more ideal than other products.
                   Moreover, the general trend with them is that as the
                   potency increases, so does the ratio between getting
                   fucked up and ODing. In a certain sense, by providing
                   this product, a dealer would be offering a safer,
                   cleaner, healthier alternative to the shit on the
                   street -- you just might be *saving* lives! ;) In any
                   case, the amount of impurities would be greatly
                   diminished (let's not get nuts here; nobody'll get any
                   humanitarian awards for distributing synthetic smack,
                   even if it meant less overdoses, which is certainly
                   debatable!)

                   BootieRocket has the right idea here of what could be
                   done. This idea also came to me. Yes, Bootie, we are
                   sick. Sick, sick, sick.

                   I have to say that what Icekat is saying is true --
                   what he described is a textbook example of an opiate
                   overdose. However, I'd also add that it's no more
                   dangerous when it comes to dose-sizing than heroin --
                   in fact its somewhat safer. A massive dose of just
                   about any opioid agonist will give the effects that
                   Icekat described.

                   Naloxone is not something you want to give to heroin
                   addicts. Wanna see a pretty freaky death? Watch what
                   happens when you give 'em an opioid antagonist --
                   "landflounder" is the name that comes to mind
                   immediately.

                   Anyways, this would be a great way of putting certain
                   countries out of business (or at least give them a run
                   for their money)-- Burma, Nigeria, Laos, Afghanistan
                   etc. Imagine the regional chaos when the one commodity
                   that bolsters the economies and dictatorships of so
                   many parts of the world
                   becomes far cheaper and easier to make "at home" than
                   they possibly could afford to do the conventional way.

                   -drone #342

   drone 342       [Image] posted 07-26-98 06:21 PM
   Member
                   [Click Here to See the Profile for drone 342]
                   -------------------------------------------------------
                   Also, before I forget. Sasha IS NOT putting together a
                   book on this stuff -- a little German elf friend of
                   mine is. I realized that my comments might look a
                   little confusing.

                   -drone #342

   Osiris          [Image] posted 07-27-98 01:30 AM
   Junior Member
                   [Click Here to See the Profile for Osiris]
                   -------------------------------------------------------
                   Drone, people would want to do blotter smack for the
                   same reasons that people want to do blotter LSD: you
                   can be sure it isn't cut with something dangerous, you
                   don't have to stick needles in your flesh or snort/eat
                   bad-tasting powder, you can be reasonably sure that
                   the dosages are roughly the same per batch, and the
                   look of the blotter paper provides an excellent way to
                   easily determine the potency/quality of the drug and
                   which batch it came from. You just suck on a tiny
                   piece of tasteless blotter paper for half an hour and
                   then spit it out.

                   Suppose you mixed your fentanyl with mannitol, like
                   you said. Can you be sure that there aren't any
                   isolated bits of pure fentanyl that didn't get
                   adequately mixed? Everyone, no matter how competent,
                   makes a mistake every now and then. Can you vouch for
                   the cutters farther down the line as well? Or suppose
                   I don't like to snort or slam mannitol or other filler
                   substances and I am used to purifying my street shit
                   before I use it. I can't do that with fentanyl because
                   I'll be lucky if I can *see* the pure drug when all
                   the cut is gone!

                   Although I am not into opiates, I would probably try
                   fentanyl on blotter (once) if it was offerent to me.
                   There is NO FUCKING WAY IN HELL I would ingest
                   fentanyl in powder form. Too risky, especially
                   considering that it looks much easier to make fentanyl
                   than LSD and therefore the competence of the cooker
                   could easily be much lower. If you were the chemist
                   I'd probably trust you to have done things correctly,
                   but out on the street you don't usually know these
                   things and the risks are simply too great.

                   As far as the ED/LD ratio, is it high enough that if
                   someone slams a couple mg of powder which is 90%
                   fentanyl instead of 0.5% (or whatever) they won't die?
                   I doubt it, although you are the expert here. This
                   could easily happen if the chemist lets any pure
                   product get out of his lab and it is cut improperly by
                   some know-nothing backstreet dealer. Thus, your
                   chemist has to cut the shit out of his stuff before he
                   sells it, thus multiplying enormously the quantities
                   of material he has to move and thereby negating one of
                   the few things that work in a chemist's favor - that
                   he can sell pure product in a less bulky form.

                   I don't mean to rain on your parade and you are the
                   expert on the drug itself and I know nothing about
                   fentanyls except what you have posted on The Hive, but
                   I honestly don't see distribution on anything but
                   blotter as being workable. With blotter the chemist
                   has the hassle of having to prepare all the doses
                   himself, but at least he isn't leaving it up to people
                   who either don't know or don't care about how to
                   properly handle such incredibly potent drugs.

                   You have let the cat out of the bag with your detailed
                   new methods of fentanyl production. If your methods
                   are as easy as you say they are, they will leave the
                   Hive and show up on the street because the smack
                   market is so very lucrative. I would hate to have this
                   new market start off with hundreds of OD deaths before
                   a safe way of ensuring dosage consistency starts being
                   used. If the people that are undoubtedly reading this
                   right now and are planning to set up fentanyl labs
                   start from scratch with use of blotter paper as a dose
                   distribution mechanism, hopefully those hundreds of
                   ODs will never have to happen.

                   Fentanyl chemists/dealers will certainly not win any
                   official humanitarian awards, but if they can convince
                   hardcore addicts to switch from AIDS-spreading needles
                   to harmless blotter tabs, I think a great good will
                   have been done. As well, if tens of millions of doses
                   of fentanyl can be cooked up without LSD-level
                   difficulty, the overall street price should come WAY
                   down due to dealer competition and maybe more addicts
                   will be able to afford their fixes without having to
                   make a living as thieves, dealers or prostitutes. I
                   think those are quite noble goals, as is the goal of
                   taking the production of opiates (and hopefully
                   cocaine too, someday) away from third world countries
                   who cannot hope for political stability as long as the
                   incredibly lucrative drug trade poses such a pervasive
                   corrupting influence.

                   This thread is without a doubt the most important
                   topic that has yet come up on the Hive. In fact, it is
                   the most important topic I have seen come up since I
                   started reading the original alt.drugs in 1990. These
                   hyperpotent synthetic analogues of heroin and cocaine
                   have the potential to change the world to such an
                   extent that I am finding it difficult to grasp the
                   sheer scale of it. Realignment of the foundations of
                   the Heroin and Cocaine trade will topple governments
                   and criminal empires.

                   Given that what is said on The Hive almost certainly
                   makes it way to the ears of those who control these
                   empires, they'll certainly perceive you as a threat to
                   their profits and try to eliminate you and anyone else
                   you are working with before you can make any further
                   advances or publish that book.

                   You had better make sure that your internet anonymity
                   is absolutely uncompromiseable. Better get a Nymserver
                   account from the Lycaeum instead of your current
                   hotmail account, and invest in a subscription to a TCP
                   anonymizer while you are at it. You need to assume
                   that these people have the resources to buy phone taps
                   and traces, pay hackers to sniff packets everywhere
                   looking for the string "Drone 342" and to break into
                   any systems that they need to to acquire this
                   information. They could bribe or threaten the managers
                   of Wolfe.net (The Lycaeum's upstream internet service
                   provider) to allow them to sniff every packet that
                   enters or leaves the Lycaeum. They could do the same
                   to Hotmail, which logs all TCP connections.

                   These people will not be worried about their evidence
                   being admissible in court, they will not have to
                   operate within the law to get their information, and
                   they have enough money to buy God. They won't want to
                   arrest and prosecute you, they will want to kill you.
                   And right now you are the single biggest threat to
                   their money and power.

                   If the speculators about the CIA's drug running are
                   correct, this will also put a severe crimp in *their*
                   cash flow, and if you don't want to piss of the drug
                   cartels, you REALLY don't want to piss of the spooks.
                   The spooks can find anyone, anytime, anywhere and take
                   them out with surgical precision. That is their job.
                   And they work hand-in-glove with the NSA, who analyze
                   every single packet that flows over the internet.
                   Worldwide. They are almost certainly going to read
                   this. Hi, guys!

                   No, I am not posting this in the middle of a meth
                   psychosis. I am completely sober. If you aren't scared
                   yet, you are a fool. I am pretty fucking scared
                   myself. If you continue to work on making syntheses of
                   cocaine and heroin analogues easier, I suggest you cut
                   all societal contacts and move to somewhere very
                   remote to continue your work. You MIGHT be safe enough
                   if you use the Nymserver and a TCP anonymizer, but I
                   can't guarantee that those resources haven't been
                   co-opted by the spooks as well.

                   Good luck in whatever you choose to do, Drone. You'll
                   need it.

                   First off, thank you for the kind words. I've given
                   this action a lot of thought, and I felt it very
                   necessary to the right thing by letting the world
                   know.

                   You said:

                   "Fentanyl chemists/dealers will certainly not win any
                   official humanitarian awards, but if they can convince
                   hardcore addicts to switch from AIDS-spreading needles
                   to harmless blotter tabs, I think a great good will
                   have been done. As well, if tens of millions of doses
                   of fentanyl can be cooked up without LSD-level
                   difficulty, the overall street price should come WAY
                   down due to dealer competition and maybe more addicts
                   will be able to afford their fixes without having to
                   make a living as thieves, dealers or prostitutes. I
                   think those are quite noble goals, as is the goal of
                   taking the production of opiates (and hopefully
                   cocaine too, someday) away from third world countries
                   who cannot hope for political stability as long as the
                   incredibly lucrative drug trade poses such a pervasive
                   corrupting influence."

                   You also said:

                   "These hyperpotent synthetic analogues of heroin and
                   cocaine have the potential to change the world to such
                   an extent that I am finding it difficult to grasp the
                   sheer scale of it. Realignment of the foundations of
                   the Heroin and Cocaine trade will topple governments
                   and criminal empires."

                   ...And that is exactly why I had to let this
                   information out. I couldn't have said it better.

                   Yes, I am concerned a bit for my own annonymity,
                   privacy, and freedom. However, I've ALWAYS posted from
                   public terminals annonymously. While the
                   Powers-That-Be could certainly find me out if they
                   REALLY tried, I'll just take my chances. If this
                   spreads, it was worth it. If not, then I'm safe.

                   Anyways, back to nuts-and-bolts. Originally, I was
                   skeptical of the blotter packaging idea, but now I see
                   its advantages. While I'll stand by powder for
                   personal snortin' reasons, blotter is the way to go
                   for "The Masses". For safety, eating the shit is best,
                   but eating it will pretty much eliminate The Rush --
                   the whole point to smack in the first place! It also
                   means feeling A LOT sicker. The reason people snort
                   and shoot smack is because the reward is immediate and
                   overpowering. With eating, you have to wait a bit, and
                   why wait? However, by soaking the blotter tab in 0.5
                   mL of H2O, you have your fentanyl in shootable form
                   (or a sort of nasal spray.) This means that this form
                   would be neatly dosed -- far moreso than conventional
                   H, and guarunteed uncut. Such a form would have its
                   own sort of mark of quality, and would ensure a
                   greater degree of safety for the user.

                   -drone #342

   ketone          [Image] posted 07-30-98 10:36 PM
   Member
                   [Click Here to See the Profile for ketone]
                   -------------------------------------------------------
                   Drone: the birth of a new designer drug ;-)

                   Excellent work...thanks for sharing and I commend you
                   for your guys and hard work!

                   -ketone

   Osiris          [Image] posted 07-30-98 11:51 PM
   Junior Member
                   [Click Here to See the Profile for Osiris]
                   -------------------------------------------------------
                   Drone, you are a man of conviction. Such are rare in
                   today's world, especially among drug chemists (not to
                   suggest that you are one of those, just a random point
                   y'know). I admire your courage.

                   Good to see that you are taking your internet security
                   seriously. I guess I went a little bit overboard with
                   the paranoia in my previous post, but I thought about
                   it a bit and came to the following conclusion: drug
                   lords probably won't have the technical acumen to be
                   able to track you down if you take precautions (and it
                   sounds like you are), and if the spooks wanted you
                   you'd already be dead. Besides, like you said, all
                   that fentanyl stuff is already out there in the
                   literature, right? Whacking you wouldn't solve
                   anything. But it will be very interesting to see what
                   the cartels will do when fentanyl starts hitting the
                   streets. Will they cut their prices? Will they give
                   up? Will they start producing fentanyl themselves?
                   Interesting times a-comin.

                   I like your idea about treating the blotter tabs as a
                   universal dose "package". The nasal spray idea is
                   killer! People could "shoot up" in public and no one
                   would know! You could maintain a habit and still have
                   a normal life - just tell everyone that you have
                   chronic sinus problems |->. I have heard of people
                   doing this trick with cocaine in saline solution - one
                   puff up each nostril and you have the equivalent buzz
                   of a couple cups of coffee, without the jitteriness of
                   caffeine and without a gutful of bitter liquid. Less
                   addictive than snorting lines or smoking base, too -
                   efficient doasge titration is a major key to avoiding
                   tolerance and addiction.

                   Now, the blotters will need to be printed with a
                   distinctive logo to eliminate any possibility of
                   confusion with LSD tabs. I suggest a little needle -
                   that should get the point across |->. The logo should
                   be sized to fit on one tab so if the tabs are broken
                   up and somehow mixed up with LSD tabs, they can still
                   be readily identified. That is probably pretty
                   unlikely, but better safe than sorry. The blotter
                   pattern could be customized on a per-batch basis by
                   varying the color and/or color pattern of the
                   background and/or the logo.

                   Junkies have historically looked down on psychedelic
                   drugs and LSD in particular. Given this, it'll be
                   funny as hell to see fentanyl users saying things like
                   "man, those aqua tabs were the BEST! They were soooo
                   clean..." or calling certain batches "triple-dipped"
                   |->.

   Rhodium         [Image] posted 07-31-98 08:31 AM
   Administrator
                   [Click Here to See the Profile for Rhodium]
                   -------------------------------------------------------
                   When will we get a step-by-step "recipe" for the
                   production of OTC fentanyl analogs here? Such a text
                   would get a special place on my chemistry page. It is
                   always fun to change the world as we know it ;)

   Bright Star     [Image] posted 07-31-98 09:08 AM
   Member
                   [Click Here to See the Profile for Bright Star]
                   -------------------------------------------------------
                   Thank you drone for not being scared off. Osiris put
                   the 'willies' in me for a while... but after all, the
                   information should be available. But then again, I'm
                   the paranoid type.

                   And even if these analogs become available... It
                   definatly would be a liquid, with the fentanyl
                   dissolved in it. A little shacking and everyone is
                   assured of a common dosage.

                   Bright Star

   Lump            [Image] posted 07-31-98 04:38 PM
                   [Click Here to See the Profile for Lump]
                   -------------------------------------------------------
                   Hope you guys make this a reality. Well do I remember
                   the last big batch of fentanyl analogues to hit the
                   East Coast. It was around 1992/93, and I believe the
                   material was 3-methyl-fentanyl. It was MUCH better
                   than plain vanilla fentanyl -- lasted every bit as
                   long as heroin and felt identical from rush to nod to
                   dopesickness. The stuff was all over the streets for
                   awhile and killed a couple of friends of mine. IT
                   CANNOT BE CUT IN THE USUAL WAYS WITH POWDER. I was
                   very happy to see the above suggestion of blotter, as
                   I'd been thinking of that since those noddy days.

                   By the way, does anyone know anything about George
                   Marquart (sp??). I know he's rotting away for
                   producing much of the super-fent this country has
                   seen, but never learned much about him.

   Osiris          [Image] posted 07-31-98 11:49 PM
   Junior Member
                   [Click Here to See the Profile for Osiris]
                   -------------------------------------------------------
                   I read about Marquat in Newsweek when he was busted.
                   They said he was supplying the entire east coast with
                   fentanyl, was a reclusive super-genius chemist, and
                   acted alone. Wierd guy - when the judge asked him what
                   type of chemist he was, he said "clandestine" |->. I'm
                   sure that didn't reduce his sentence any...

   Cyclops         [Image] posted 08-03-98 09:51 AM
   Member
                   [Click Here to See the Profile for Cyclops]
                   -------------------------------------------------------
                   Funny you should mention Marquart. He was on an
                   episode of "The Justice Files" just last weekend. Very
                   unapolgetic too, he was. The producers of the show
                   called him a mass murderer...such audacity! He was
                   givin' the people what they wanted. Another featured
                   on the same show was J. Dahmer, one who gave nothing
                   to anyone, while taking all. Shameless non-sequitur.

   drone 342       [Image] posted 08-03-98 10:27 PM
   Member
                   [Click Here to See the Profile for drone 342]
                   -------------------------------------------------------
                   Rh,

                   A fentanyl synth with all its gory details is
                   underway. Puttin together something as involved as a
                   fentanyl "recipe" is hard work, and takes a lot of
                   time -- especially now that I don't have OCR
                   capabilities anymore! Originally, this was something I
                   was hoping to have published, and I'm still thinking
                   about it.

                   I've managed to compile information that has eluded
                   almost everyone, and it does feel a little wierd just
                   *giving* it away. Still, my beliefs drive me to do
                   something liek this. This whole writing process may
                   take a while.

                   -drone #342

   Shaft           [Image] posted 08-06-98 01:55 AM
   Junior Member
                   [Click Here to See the Profile for Shaft]
                   -------------------------------------------------------
                   Drone 342:
                   I feel that it may not be my place to say, but giving
                   this recipe away is a very
                   generous act. Alot of people harbor the
                   idea that there is a marked line between
                   opiates and other drugs due to their
                   strength, and possibility of withdrawls
                   or whatever.
                   So a bold act could be to publish
                   this book on "hard" drugs, and
                   distribute recipes freely on the fentanyl analogues.
                   It's definately not my place to say, but I say go for
                   it. I, for one,
                   think maybe a little segment could
                   be set aside for synthesis of these
                   compounds; with troubleshooting tips, recipes, and
                   further.

   saint_nicholaus [Image] posted 08-10-98 11:37 AM
                   [Click Here to See the Profile for saint_nicholaus]

                   -------------------------------------------------------
                   what up gang? short reply on blotter paper issue. if
                   fentanyl is water soluble you could drop blotter in a
                   rig and go to it i have seen it done with LSD and
                   DH2O. onset was instintaneous or about 3 seconds,
                   duration of peak was diminished to about 4 hours from
                   8, affect still hung out for about 24 hours such as
                   dialated pupils and general tweeked pespective. chris.

   Kaff            [Image] posted 08-20-98 03:36 AM
   Member
                   [Click Here to See the Profile for Kaff]
                   -------------------------------------------------------
                   I know absolutely nothing about fentanyl anoalogs in
                   fact I never even heard of them before, but they sound
                   really incredible. I never knew that there are
                   synthetic drugs stronger than heroin and cocaine. Yes,
                   definitely a great idea to get recipes for this. I
                   think also we should work on the microwave chemistry
                   aspect, as mentioned on Rhodium's page. Microwaves
                   seem to have the potential to increase yields and save
                   time. How about a bunch of chemists collaborating on a
                   really thick book- the drug version of "The Joy of
                   Cooking". A book the size of a big real cookbook.

   drone 342       [Image] posted 08-22-98 05:28 PM
   Member
                   [Click Here to See the Profile for drone 342]
                   -------------------------------------------------------
                   Progress report:

                   This synthetic description is taking way too much
                   time. However, progress is being made, and new
                   chemical insights are being discovered.

                   Yes, fentanylsare pretty amazing. However, these still
                   aren't the strongest recreational drugs of all; in my
                   studies I've seen a few things active at the
                   sub-nanomolar level that may or may not be worth
                   investigating. Can't remember much about these
                   chemicals, but I'll dig through my notes on it.

                   -drone #342

   Kaff            [Image] posted 08-22-98 11:04 PM
   Member
                   [Click Here to See the Profile for Kaff]
                   -------------------------------------------------------
                   Imagine using genetic engineering to add the
                   drug-components from marijuana or opium poppies to
                   other plants like apple trees or tomatoes so we'd have
                   fruits and vegetables containing THC and opium.

   Piglet          [Image] posted 09-02-98 05:45 AM
   Member
                   [Click Here to See the Profile for Piglet]
                   -------------------------------------------------------
                   D342 & Shaft: Direct yourselves to US patent 3,905,981
                   which describes the cleavage of tertiary amines and a
                   route to replace the N-Methyl with other substituents
                   at 75% yield. -OH groups need to be protected.
                   As I see it.

                   1. Convert codeine to hydrocodone a la rhodium method.

                   2. Replace N-Methyl with N-phenyl ethyl using methyl
                   chloroformate (DIY from ethylene glycol and phosgene
                   (careful!!).
                   3. Remove methyl ester with HBr in CH3COOH.

                   This should yield about 30%. Your product is about 100
                   times stronger than morphine. As strong as 3-methyl
                   and somewhat simpler to do (I guess).

                   Criticism please,
                   Piglet :)

   Piglet          [Image] posted 09-02-98 08:45 AM
   Member
                   [Click Here to See the Profile for Piglet]
                   -------------------------------------------------------
                   Actually, I think that there are n-substituents that
                   are stronger than PE. Rhodium's page has links to some
                   of the research centers for these things.
                   Also, I think replacing that 6 =O group with other
                   funky things has quite an impact on the agonist
                   strength. =CH2 is 80 times stronger than -OH but a
                   bitch to get in. I seem to remember than amino groups
                   appear in some of these things. Check the RBI...

                   Piglet :)

   drone 342       [Image] posted 09-02-98 07:49 PM
   Member
                   [Click Here to See the Profile for drone 342]
                   -------------------------------------------------------
                   Piglet,

                   Thanks for the tip on the tertiary amines
                   substitution; I'll give that a thorough investigation.
                   Right now I'm looking into just that issue, since when
                   Tropinone does what I said it would do, there is a
                   place in the mechanism where it does violate Brett's
                   rule -- though there are examples of tropinone
                   methyliodate succesfully getting away with doing such
                   a thing. More research needs to be done here.

                   -drone #342

   Kaff            [Image] posted 09-03-98 04:20 PM
   Member
                   [Click Here to See the Profile for Kaff]
                   -------------------------------------------------------
                   Strike says the war is over on the back cover of Total
                   Synthesis. The war isn't ever over but it would be
                   nice to have a book on the more advanced drugs such as
                   China White. Just out of curiosity, what are the main
                   precursors of this dessert? Sounds better than Russell
                   Stover-Fanny Farmer- Whitman-Laura Secord-Tobler Swiss
                   milk chocolate!!!

   Piglet          [Image] posted 09-05-98 08:40 AM
   Member
                   [Click Here to See the Profile for Piglet]
                   -------------------------------------------------------
                   Could I also suggest some bits?

                   1. Naloxozine 'potent u1 receptor antagonist'. I won't
                   bore you with the full name but imagine 2 Oxymorphone
                   molecules with an N-allyl group (antagonist) on each N
                   and the two are bonded by a hydrazide at the 6
                   positions. I wonder how srtong an agonist this would
                   make? Not impossible to make...

                   2. Endomorphin 1/2 . these are 6 peptides long with an
                   amino at one end. How the fuck do you build these
                   things?
                   Also, TAPP is another strong agonist of a similar
                   makeup.

   Piglet          [Image] posted 09-06-98 08:00 AM
   Member
                   [Click Here to See the Profile for Piglet]
                   -------------------------------------------------------
                   D342:
                   You know anything about Clonitazine and Etonitazine
                   'potent u opioid receptor anonist; narcotic analgesic'
                   Merck12th edition No3929.
                   I can't find anything about this unique class of opiod
                   analgesic.

                   Ideas:

                   1. Ever checked out the structure of diphenhydramine,
                   common antihistamine.
                   If you cleave the ether, you end up with to very good
                   building blocks for methadone type analgesics, I
                   should think.

                   2. Ever checked out Loperamides structure. It's got
                   the meperidine skeleton right inside and I think the
                   amide is fine (similar to the one in dextromoramide)
                   and although it lacks a methyl side-chain, other
                   powerful drugs are the same (piritamide, diphenoxyl
                   butyrate,benzitramide) and although it has a bulky
                   group of the benzyl group (like piritimide and
                   benzitrimide again, as well as difenoxin) it SHOULD
                   still have quite some activity. I guess that the
                   alcohol prevents it crossing the blood-brain barrier
                   and the Cl makes it bind to k receptors more (just
                   like haloperidol).
                   a. Make ether from alcohol (protection).
                   b. Grignard off the Cl. The amide SHOULD stay put, if
                   you remember our discussion of some months ago...

                   3. Cocaine analogues. I notice in the RBI lots of
                   4-halo cocaine derivitives which although not
                   scheduled, are marked as 'NO telephone orders taken
                   for this compound, NOT for sale in europe'.

                   a. Make para-halo benzoic acid via sandmayer procedure
                   (swap the Cl by adding KI or KBr) or the Gatterman
                   synthesis using butyl nitrate and CuX2 which MIGHT be
                   better.

                   b. DIY some acetic anhydride and make the substituted
                   benzoic anhydride from it.

                   c. Buy some coke, clean and degrade to ecgonine.

                   d. Make coke analogue with i) bubble HCl gas through
                   methanol solution of ecgonine.
                   ii) Add benzoic anhydride.

                   See BER 89,679(1956) or simpler still, PC by MVS Page
                   142.

                   Of course, you need sodium flouroborate or HF to make
                   the flouro-. I'm not too keen on messing with them!

                   All the best,
                   Piglet :)

   Piglet          [Image] posted 09-06-98 08:05 AM
   Member
                   [Click Here to See the Profile for Piglet]
                   -------------------------------------------------------
                   PS the PABA (Para Amino Benzoic Acid) is another diet
                   supplement which at my hippy shop is 2 shelves below
                   the B1 ;)

                   I'm gonna drive you crazy with mad precursor ideas! I
                   reckon if I throw enough at you, something will stick!
                   Mostly it's vitamins right now.

   A N Onymous     [Image] posted 09-14-98 04:11 AM
   Junior Member
                   [Click Here to See the Profile for A N Onymous]
                   -------------------------------------------------------
                   Drone342 I noticed that you and Piglet discussing the
                   Benzimidazoles & wondered if a little bit of
                   information might help you both. I have seen on the
                   shelves of a US photographic supply outlet the sale of
                   '5-Nitro Benzimidazole Nitrate' which I wondered if it
                   might useful for you to know.
                   It cost $95 for 100g which seems pretty cheap if you
                   asked me.

                   If/When I get more information I will post. I use my
                   friend's computer so it takes me time to reply.

   Piglet          [Image] posted 09-14-98 04:33 AM
   Member
                   [Click Here to See the Profile for Piglet]
                   -------------------------------------------------------
                   D342: Direct yourself to US Patent 5,262,428 which is
                   a pretty cool thing about the coke analogues.
                   I found this whilst hunting for the term 'Mazindol'
                   which is a diet drug. I still can't find any details
                   except for it affects the dopamine pathway in a
                   similar manner...

                   Piglet [Image]

                   PS: AN: Got any synth references. I can't find out if
                   it's useful until I know how the stuff is made!

   guesswork       [Image] posted 11-23-98 06:29 PM
   Member
                   [Click Here to See the Profile for guesswork]
                   -------------------------------------------------------
                   Hey kids. Nobody has posted here in a while, but I
                   used to know lots about fentanyl derivatives, so I
                   figured I'd shout in. 3-methyl-fentanyl and
                   alpha-methyl-fentanyl are the most powerful and are
                   relatively equally powerful. In terms of dose
                   equivalents, they are much more soluable than heroin
                   at room temperature.

                   But to those of you who haven't heard of fentanyl
                   derivatives before, don't think drone discovered
                   something new. They've been around since the early
                   80's. When they first came out people were OD'ing but
                   no forensic lab in the nation could detect the
                   fantastically low doses of these fentanyls it takes to
                   kill you. There was only 1 lab in the world then that
                   was high tech enough to sniff out 3-methyl-fentanyl
                   overdose levels. Some Dow(?) chemist was arrested in
                   85(?) for trying to sell one ounce of the better
                   n-methyl-fentanyl. His asking price was 1/2 million.
                   At the time that much heroin equivalent was worth $13
                   million.

                   But I seriously wouldn't even dream about making a
                   drug whose overdose rate is 1/2 a grain of sand.
                   Careful now.

   beagle_boy      [Image] posted 11-23-98 08:27 PM
   Member
                   [Click Here to See the Profile for beagle_boy]
                   -------------------------------------------------------
                   I'm a little late getting in on this conversation, but
                   in rereading this excellent thread I have a few
                   comments.

                   Regarding the talk of succindialdehyde, it would be
                   best to avoid it altogether and use the
                   succindialdehyde equivalent
                   2,5-dimethoxytetrahydrofuran, which is avail. OTC from
                   photo supply places BTW. Or even better go through the
                   nitrone route to cocaine. Are you aware of this route?

                   Piglet: I'm not sure what turned up on your search for
                   Mazindol info, but I'm pretty sure that it doesn't
                   have any fun potential. It is interesting that this
                   cpd that is a decent dopamine uptake inhibitor and
                   still isn't worthwhile.

                   I've always been amazed that fentanyl doesn't turn up
                   more on the street considering how phenominally easy
                   these analogs are to make. Maybe its the complications
                   with dilution.

   Piglet          [Image] posted 11-24-98 04:06 AM
   Member
                   [Click Here to See the Profile for Piglet]
                   -------------------------------------------------------
                   guesswork: Firstly, they are NOT the most powerful
                   fentanyl derivitives by a factor of about 30.
                   Carfentanil, Lofentanyl, remifentanyl and a HOST of
                   others. 3-methyl is 125x morphine, carfentanil is
                   4000x morphine. Get the picture? One oz of 3-methyl
                   equates to 1.1Kg smack. Even at street prices thats
                   only about £90000. Bulk, it's about £45000.
                   Drone never say's it's a new drug,although it IS an
                   analoguge. The point is a more OTC synthesis. We can
                   ALL read the patents. Doesn't mean we can actually
                   make it?
                   By the way, what is N-methyl fentanyl supposed to be?
                   If either of the 2 nitrogen's has a methyl group, it
                   isn't a fentanyl. Unless I'm missing something?

                   Beagle_boy: well, Mazindol IS controlled and it's
                   structure IS a rigid-body-PEA? That Cl might be
                   removed to make something good?

                   Piglet [Image]

   beagle_boy      [Image] posted 11-24-98 08:41 AM
   Member
                   [Click Here to See the Profile for beagle_boy]
                   -------------------------------------------------------
                   I don't see Mazindol as being worthwhile in and of
                   itself or as a starting material. It is curious that
                   it is a CS. I've seen a study where monkeys were
                   trained to shoot up speed and when the speed was
                   replaced w/ mazindol the monkeys got really pissed off
                   and said that mazindol has no abuse potential and is
                   no fun at all (OK, so I'm paraphrasing what the
                   monkeys said).

                   I guess that the DEA wants any appetite supressant to
                   be a CS whether it has abuse potential or not. Witness
                   the recent classification of "Meridea", another diet
                   aid that supposedly has little to no abuse potential.
                   But are you saying that Mazindol is a CS in UK? I
                   wonder if independant studies of abuse potential were
                   done.

   Piglet          [Image] posted 11-24-98 09:12 AM
   Member
                   [Click Here to See the Profile for Piglet]
                   -------------------------------------------------------
                   Yes, it is controlled, and as I said, that chlorine
                   group needs lopping off in my opinion. Without that I
                   reckon it would be pretty active. How to make it,
                   though?

   beagle_boy      [Image] posted 11-24-98 10:47 AM
   Member
                   [Click Here to See the Profile for beagle_boy]
                   -------------------------------------------------------
                   Why do you reckon that it would be any more active w/o
                   the Cl? This cpd acts in a different manner than
                   amphet. Attempts to extrapolate SAR info from 1 class
                   to the other are useless IMHO.

   Piglet          [Image] posted 11-24-98 10:52 AM
   Member
                   [Click Here to See the Profile for Piglet]
                   -------------------------------------------------------
                   Different manner of action? Pray tell?

   beagle_boy      [Image] posted 11-24-98 11:12 AM
   Member
                   [Click Here to See the Profile for beagle_boy]
                   -------------------------------------------------------
                   Mazindol interacts with the dopamine transporter
                   receptor at a site different from cocaine or BTCP,
                   blocking reuptake. Amphetamine also inhibits the
                   reuptake of amphetamine by interaction at another
                   dopamine receptor site but probably more importantly
                   it acts as an indirect DA agonist by stimulating the
                   release of dopamine.

   beagle_boy      [Image] posted 11-24-98 11:13 AM
   Member
                   [Click Here to See the Profile for beagle_boy]
                   -------------------------------------------------------
                   Whoops, typo. That should be "Amphetamine also
                   inhibits the reuptake of dopamine...."

   drone 342       [Image] posted 11-24-98 05:26 PM
   Member
                   [Click Here to See the Profile for drone 342]
                   -------------------------------------------------------
                   I got bad news. The reason you haven't seen a FAQ yet
                   on tropinone-derived fentanyls is that the reaction
                   with tropinone doesn't yield well (bad, bad yeilds
                   (5-10%), but a product none-the-less.) Still, by using
                   commercially available methylpiperidone instead, this
                   method works well. Sadly, its not 100% OTC.

                   -drone #342

   Kaff            [Image] posted 11-30-98 12:44 AM
   Member
                   [Click Here to See the Profile for Kaff]
                   -------------------------------------------------------
                   What's wrong with a yield of 5-10% on a product that's
                   at least 100 times stronger than heroin? An FAQ would
                   still be good just for the interesting read.

   Kaff            [Image] posted 11-30-98 03:43 AM
   Member
                   [Click Here to See the Profile for Kaff]
                   -------------------------------------------------------
                   TEST after I put on a post on this thread and returned
                   to the Chem Discourse board and clicked on this topic
                   (a gift from drone to dea) only the first 10 posts of
                   it showed up. I kept clicking back and forth but
                   didn't get the whole thread, but when I clicked on
                   "post reply" I did get the whole thread.

   Free Radical    [Image] posted 03-28-99 07:49 PM
   Member
                   [Click Here to See the Profile for Free Radical]
                   -------------------------------------------------------
                   I guess you can still post here.
                   If anybee can find this thread within a thread.

   Slappy          [Image] posted 04-04-99 06:32 AM
   Member
                   [Click Here to See the Profile for Slappy]
                   -------------------------------------------------------
                   Drone-

                   What is the status of that paper? Are you still
                   working on it, or have you given up all together?

                   -S

                   PS- Take a look at the photosynthesis thread on the
                   novel forum.

   niteflier       [Image] posted 04-04-99 03:42 PM
   Member
                   [Click Here to See the Profile for niteflier]
                   -------------------------------------------------------
                   Drone...how is this going??? While not personally
                   interested in these compounds I share your conviction
                   that this info should be very public. Publishing is an
                   exellent idea... I would help in the publishing part
                   any way I could...It would change the world as we know
                   it...


- - - - - 

Drone, you are a hero to any hard-core opioid aficionado!
Hey, everybody!

DopaMan here. Sorry for just suddenly contributing here out of the blue, but I
know a lot about fentanyls, and have had personal experience.
I must disagree with the potencies listed before.

Remifentanil, which is new on the market as an anesthetic/analgesic, like
alfentanil, is only about half, to one-fourth, as potent as fentanyl, depending
on the patient and the circumstances of use. It is approximately equivalent in
potency to alfentanil. This information was furnished from the 1998 PDR, as well
as other sources.

Next, fentanyl is approximately 100 to 150 times as potent as morphine, some say
80, some say 200. I say 100-150 times as potent. I, personally, have had
fentanyl five times, for a total of 10 injections. I have never been so high as
the first time they gave me fentanyl. Indeed, it produces the most euphoria of
any opioid, or drug, for that matter, that I have ever had. Much more so than
morphine, and the rush, though it takes longer by about twenty seconds, to hit
you than morphine, is sublime. Hence, Sublimaze! II never had any breathing
trouble, and I was given nearly anesthetic doses on a few occaisions (one time
as high as 0.2 mg, as the normal dose is about 0.025-0.05 mg. I did pass out
when they gave me propofol on top of that and the Versed (midazolam HCl), but
only because of that damn propofol! I think that breathing trouble must have
been a unique, idiosyncratic reaction, as it's called. Something unusual, and
unique to IceKat, or to a small group of the population. Also, nausea is unusual
for fentanyl, although itching is a constant for all opioids. I had a bit of a
problem with that when I first had fentanyl. I don't think the therapeutic ratio
of fentanyl is actually that much higher than H, but I could be wrong. They can
use it as an anesthetic by itself, with oxygen, which they sometimes do for
delicate triple bypass, and other open heart procedures, which they certainly
couldn't do with heroin, but they dosage is crucial, with higher concentrations,
and naloxone must be onhand.

By the way, there are no bad effects from being administered naloxone by itself.
Check the PDR. One can be given nearly 1000 times the normal dose with only a
sense of malaise resulting. It would, of course, make it awful for someone in
pain, as they would need their endorphins to work, which it would block
effectively, but, otherwise, it's pretty-well-tolerated shit, unless you happen
to be opioid-dependant, in which case you would spontaneously withdraw. I'm not
sure where a person would get the idea it is somehow a nasty substance, aside
from the fact that it'll ruin your high.

Next, sufentanil--
I've never had sufentanil, but I know, once again from a PDR (1994), that it's
7-10x more potent than fentanyl (so, about 1000 x morphine, give or take).
I happen to know that TMF, or 3-methylfentanyl, used as either the hydrochloride
or isothiocyanate, is about 5,500 x as potent as morphine, compared to the
2000-3000 times morphine potency of AMF, or alpha-methylfentanyl hydrochloride.
It is not only 150 times as potent as morphine--that's fentanyl's potency. The
reason people make TMF, or did so much in the eighties, is it affords much, much
greater potency over original fentanyl. I have read experimental anesthesiology
books, and have this on good authority.

Lofentanil is about 4000-8000 times as powerful as morphine, second only to its
predecessor, carfentanil, the ultimate opioid. This seems strange to me, as it
is the 3-methyl, levorotatory analogue of carfentanil, so it seems like it
should be more potent. I guess these rules are sometimes wacked.

Carfentanil is one of the two most potent drugs ever conceived. I checked this
one out in a vet's reference, as it is used now in place of etorphine HCl, in a
liquid for darts called Wildinil. According to the reference, and a few other
books I've looked in, it has a clinical potency of 10,000 times that of
morphine; yes, seriously. I have it on good authority that this is the case.
Check it out. It's true. It may actually be the most potent drug on the planet.
It is considered to be an exceptionally powerful, euphoric, mu agonist opioid of
the morphine/fentanyl type, but it is so potent that it kills at smaller doses
than anything else in the known world. For example, it is more lethal to spill
the solution on you're skin, or inhale it,  than VX, for fuck's sake! It, or
this one other opioid with a long numeric name starting with the letters and
numbers Ro-18...something, I can't remember which, was listed in the Guinness
Book of World Records, about ten years back, when they actually had a more
extensive range, and a drug/chemical extremes section, as the most lethal
substance on earth, due to its extreme potency. It and carfentanil are one in
the same, I understand. They are both at least 10,000 times morphine potency. A
shoe box full of the stuff would supply the entire double continent of
North/South America with narcotizing doses of an opioid every day for months!
Imagine making a key-low (aka kilo) of the stuff. You would be set for 10
lifetimes, as long as you had good distributors, and as long as you weren't
propositioning African-American employee's, like at DuPont, where that one
entrepreneuring chemist who made all that TMF, tried propositioning the janitor,
because of ridiculous stereotype beliefs that black guys are automatically
hooked up. I would personally love to here more about the making of fentanyl
analogues from phenylpropanolamine, and what the chemical designation of that
one from tropane would be.

Lastly, that 5'-nitrobenzimidazole is something to definitely take a look at!
It could be used to make either etonitazene or clonitazene! Both are about 1500
times as potent as morphine! Etonitazene mesylate is chemically identified as
1-(beta-diethylaminoethyl)-2-para-ethoxybenzyl-5'-nitrobenzimidazole methane
sulphonate. Clonitazene is the 2-para-chlorobenzyl- analogue. They are extremely
potent. The most so of any open-chain opioids, to my knowledge. I will post
again after I research these compounds a bit more, or even before then,
as I have a few developing synthesis ideas myself. Take it easy everybody!

The high-binding-affinity superhero you know as DopaMan : ) !


