Synfacts 2021; 17(12): 1314
DOI: 10.1055/s-0041-1737090
Synthesis of Natural Products and Potential Drugs

Synthesis of BMS-986158

Philip Kocienski


BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) family of adaptor proteins that are involved in the transcriptional regulation of key oncogenes. It has entered phase 1/2a clinical trials in patients with advanced cancers and hematologic indications including ­myelofibrosis.



Key steps in the small-scale discovery synthesis of the 5H-pyrido[3,2-b]indole core of BMS-986158 are (1) the copper-catalyzed oxidative coupling of the chloropyridine C with the boronic acid D (Chan–Lam coupling) and (2) the palladium-catalyzed C–H activation reaction EF.


Publication History

Publication Date:
17 November 2021 (online)

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