BMS-820836-03 is a �Triple Reuptake Inhibitor� that regulates the uptake of serotonin, dopamine and norepinephrine, and is a potential therapeutic agent for the treatment of depression, neurophatic pain and other related neurological disorders. This presentation will focus on the evolution of the synthetic route to enable the preparation of toxicological and clinical supplies. The optimized route is convergent and features a 6-step longest linear sequence with complete regio- and enantio- control. The synthesis highlights include: the development and demonstration of a regioselective Friedel-Crafts reaction using boron-containing compounds and the development of a Suzuki-Miyaura cross-coupling including a detailed control strategy of residual oxygen levels to provide predictable performance on scale.

Process development for the preparation of BMS-820836, a triple reuptake inhibitor

248th National Meeting (2014)

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