Diversification of Pharmaceuticals via Late-Stage Hydrazination.

ABSTRACT: Developments in organic synthesis over the past century have greatly enabled the discovery of life-saving medicines. In this context, over the past two decades, palladium-catalyzed cross-coupling reactions have transformed the exploration of emerging therapeutics. However, the cross-coupling between aryl halides and hydrazine, NH2NH2, the smallest bis-nitrogen nucleophile, has been a long-standing challenge due to the reducing capacity of hydrazine and the presence of multiple N-H bonds. These advances have significantly lagged behind modern cross-coupling technologies despite the broad utility of arylhydrazines to serve as a springboard for the discovery of innovative medicines. Herein, we report a general platform for the diversification of pharmaceuticals by late-stage hydrazination. By

SUBMITTER: Zhou T 

PROVIDER: S-EPMC12362435 | biostudies-literature | 2025 Aug

REPOSITORIES: biostudies-literature