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 CÀ 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 deuteriumlabeling experiment. The gram-scale synthesis and synthetic transformations are also conducted, confirming the scalability and application value.