Palladium-Catalyzed Regioselective Insertion of Carbenes into γ-C(sp 3 )-H Bonds of Aliphatic Amines.

A migratory insertion of carbenes into distal γ-C(sp 3 )-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(sp 3 )-H bonds.