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

• DOI: 10.1021/acs.orglett.1c01725
• Publication Date: 2021-06-29T18:57:16Z
• Authors: Dinesh J. Paymode; Le Chang; Dan Chen; Binglin Wang; Komirishetty Kash...; Vijayagopal Gopal...; D. Tyler McQuade; N. Vasudevan; Saeed Ahmad; David R. Snead
• Keywords: Sequence (biology)

MMV390048 (1) 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 steps. This sequence takes advantage of raw materials used in existing etoricoxib supply chain and eliminates need palladium catalysts, were projected to be major cost-drivers.