Part 1. Discovery of ABT-199 and its First Synthetic Route<br/>The discovery of Venetoclax (ABT-199), a selective inhibitor of BCL-2 for the treatment of cancer, is presented. The biological rationale is discussed with reference to earlier BCL-2 family inhibitors. Emphasis is on the synthesis of intermediates and the final compound, with a particular focus on the key steps involving insertion of the moiety involved in driving selectivity.

Synthetic routes to Venetoclax at different stages: From discovery to early development to commercialization (part 1)

256th National Meeting (2018)

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