CCR2 is critically involved in the migration of inflammatory monocytes and has been implicated in the pathogenesis of a number of inflammatory diseases. In our own efforts to develop selective small molecule antagonists of this receptor, we previously developed SAR from intermediate 1. Presently, we describe our continued advancement of these SAR efforts through the Curtius rearrangement of 1, leading to the discovery of clinical candidate BMS-741672. The first generation synthesis of BMS-741672 will be described in detail.

Design and synthesis of 2-substituted cyclohexylaminobenzamide-derived inhibitors of CC Chemokine Receptor 2 (CCR2)

245th National Meeting (2013)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.