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

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.

Automated summary

This paper describes an approach for the synthesis of 2-acyl indolines through Cobalt-catalyzed C-H activation/[3+2] annulation of aniline derivatives and acrylates. The method utilizes a cobalt catalyst to achieve high regioselectivity in the formation of functionalized 2-acylindolines. The mechanism is investigated through KIE experiments and deuterium-labeling experiment. The scalability and application value of the method is confirmed through gram-scale synthesis and synthetic transformations.