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

A migratory insertion of carbenes into distal gamma-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.