Late-stage C–H amidation of pharmaceuticals enabled by earth-abundant Co(III)-catalysis

Abstract

A Cp*Co(III)-catalysed late-stage C–H amidation of pharmaceuticals proved viable with dioxazolones as nitrogenating agents in EtOAc. High-throughput experimentation identified mild, chemoselective and orthogonal conditions, enabling bifunctional linker installation and single-step PROTAC/biotin conjugation. This LSF approach reduces predicted PMI versus traditional routes, offering sustainable, efficient access to complex drug derivatives.