A multi-kilogram manufacturing route of AMG 986 was developed to supply initiation of human clinical trials. Process Development’s early collaboration with Medicinal Chemistry led to the discovery of an improved synthetic route to chiral sulfonamide (<b>1</b>) <i>via</i> an unprecedented stereoselective hydrogenation of a tetra-substituted olefin. This innovation enabled a new convergent route to AMG 986 which after further refinement to control impurities, isolations, and improve yields has successfully delivered over 50kg of AMG 986.

Early phase process development and scale up of novel APJ agonist AMG 986

2019 Spring National Meeting

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