Palladium-Catalyzed Selective γ-Monoarylation of Free Amines Containing Symmetric γ-C-H Controlled by a Transient Directing Group.

We developed a new transient directing group, -(2-benzoyl-4-chlorophenyl)-1,1,1-trifluoromethanesulfonamide, which can facilitate the γ-monoarylation of free amines containing symmetric γ-C-H bonds. A variety of amines containing symmetric and identical γ-C(sp)-H and γ-C(sp)-H reacted with a diverse range of aryl and heteroaryl iodides to provide γ-monoarylated products exclusively.