Highly Regioselective Synthesis of 2‐Acylindolines through Cobalt‐Catalyzed C−H Activation/[3+2] Annulation of Aniline Derivatives and Acrylates

Abstract An approach for 2‐acyl indolines synthesis through Cobalt‐catalyzed C−H activation/[3+2] annulation of aniline derivatives and acrylates is described. The method employs cobalt catalyst to afford a wide variety of functionalized 2‐acylindolines with high regioselectivity. The mechanism is investigated by KIE experiments and deuterium‐labeling experiment. The gram‐scale synthesis and synthetic transformations are also conducted, confirming the scalability and application value. magnified image