AR-C1187925 has been presented as a selective P2Y2 receptor antagonist. As this interesting substance is neither available through commercial nor non-commercial sources, a project to synthesize it was initiated at our institute in 2005.

As depicted below, AR-C1187925 is sequentially put together from four precursors: First an activated and protected uracil moiety is fused to 2,8-dimethyldibenzosuberenone. The deprotected product is then coupled with a methylfurancarboxylic acid derivative, thionated and deprotected. Finally the free acid is coupled to aminotetrazol.

The synthesis of 2,8-dimethyldibenzosuberenone proved to be less than trivial, as described in:

J. Burbiel, “On the syntheses of dibenzosuberenone and 2,8-dimethyldibenzosuberenone”, ARKIVOC (xiii) 16-21 (2006) (view as pdf (external link))

The AR-C1187925 produced in my lab is currently used in several pharmacological studies. Publication of results are currently in preparation.