Abstract:Herein, we describe the enabling synthesis of (+)-BMS-820836, a 4,7-disubstituted tetrahydroisoquinoline which was developed as a treatment for a range of neurological diseases, including depression and neurophatic pain. In order to advance the drug candidate into the Phase 1 clinical trials, an efficient and scalable synthesis was required. Three areas of improvement included the development of a regioselective Friedel−Crafts cyclization, a classical resolution for the purification of the desired enantiomer, … Show more
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