Palladium-Catalyzed C–N Bond Cleavage of 2<i>H</i>‑Azirines for the Synthesis of Functionalized α‑Amido Ketones

A Pd-catalyzed ring-opening reaction of 2H-azirines with carboxylic acids was developed. This reaction undergoes nucleophilic addition between 2,3-diaryl-2H-azirines and carboxylic acids followed by C–N single-bond cleavage and a subsequent thermal rearrangement. This method enables the rapid construction of valuable α-amido ketone derivatives with high atomic efficiency and superb functional group tolerance.本研究开发了一种钯催化的2H-氮丙啶（2H-azirines）与羧酸的开环反应。该反应先经历2,3-二芳基-2H-氮丙啶与羧酸之间的亲核加成，随后发生C-N单键断裂及后续热重排过程。此方法能够以高原子经济性和优异的官能团耐受性，快速构建具有应用价值的α-酰胺基酮衍生物。