Palladium-Catalyzed Regioselective Insertion of Carbenes into γ-C(sp³)–H Bonds of Aliphatic Amines

A migratory insertion of carbenes into distal γ-C(sp3)–H bonds of aliphatic amines has been successfully developed. The synergistic interplay among a palladium catalyst, picolinamide directing group, a carefully selected base additive, and an essential ligand proved crucial in achieving high yields. These findings hold significant value for advancing the exploration of regioselective carbene insertions into nonactivated C(sp3)–H bonds.