Mild C(sp3)−H Alkylation of 8‐Methylquinolines with α,β‐Unsaturated Carbonyl Compounds by Rhodium(III) Catalysis

Abstract A straightforward approach to the synthesis of γ‐quinolyl carbonyl compounds has been developed by a rhodium(III)‐catalyzed C(sp 3 )−H alkylation of 8‐methylquinolines with conjugated C=C multiple bonds. Remarkably, this C(sp 3 )−H functionalization proceeds under mild reaction conditions, obviates the need for external oxidants, features high atom‐economy, ample substrate scope and wide functional group tolerance. Mechanistic studies provided strong support for an irreversible C(sp 3 )−H bond activation.