Copper-Catalyzed Amination of C(sp³)–H bonds: From Anilides to Indolines

Abstract

Copper-catalyzed oxidative intramolecular cyclization of <i>o</i>-alkylated anilines via cleavage of C(sp³)-H and N-H bonds for the production of indolines is described. This approach provides a straightforward strategy for the synthesis of nitrogen-containing heterocyclic compounds through the functionalization of unactivated C(sp³)-H bonds with high site selectivity. The present catalytic system shows high preference for functionalization of unactivated C(sp³)-H bonds over C(sp²)-H bonds, leading to C-N bond formation.