Application of Vinamidinium Salt Chemistry for a Palladium Free Synthesis of Anti-Malarial MMV048: A "Bottom-Up" Approach

16 Jul 2021

Paymode DJ, Chang L, Chen D, Wang B, Kashinath K, Gopalsamuthiram V, McQuade DT, Vasudevan N, Ahmad S, Snead DR

Organic letters
PMID: 34185545

Doi: 10.1021/acs.orglett.1c01725

Photo: Dtimiraos_iStock

MMV390048 is a clinical compound under investigation for antimalarial activity. A new synthetic route was developed which couples two aromatic fragments while forming the central pyridine ring over two steps. This sequence takes advantage of raw materials used in the existing etoricoxib supply chain and eliminates the need for palladium catalysts, which were projected to be major cost-drivers.

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