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

Copper-catalyzed oxidative intramolecular cyclization of o-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.