Development of a Green and Sustainable Manufacturing Process for Gefapixant Citrate (MK-7264) Part 3: Development of a One-Pot Formylation–Cyclization Sequence to the Diaminopyrimidine Core

• DOI: 10.1021/acs.oprd.0c00246
• Publication Date: 2020-10-20T11:44:10Z
• Authors: Kallol Basu; Dan Lehnherr; Gary E. Martin; Richard A. Desmond; Yu-hong Lam; Feng Peng; John Y. L. Chung; Rebecca A. Arvary; Michael A. Zompa; Si-Wei Zhang; Jinchu Liu; Zachary E. X. Dance; Patrick Larpent; Ryan D. Cohen; Francisco J. Guzman; Nicholas J. Rogus; Michael J. Di Maso; Hong Ren; Kevin M. Maloney
• Keywords: 01 natural sciences; 0104 chemical sciences; 12. Responsible consumption

The development of a safe, robust, and efficient manufacturing route for the synthesis of diaminopyrimidine 1, a key intermediate to gefapixant citrate (MK-7264), is described. A full mechanistic u...