Easily accessible auxiliary for palladium-catalyzed intramolecular amination of C(sp²)-H and C(sp³)-H bonds at δ- and ε-positions.

An easily synthesized and accessible N,O-bidentate auxiliary has been developed for selective C-H activation under palladium catalysis. The novel auxiliary showed its first powerful application in C-H functionalization of remote positions. Both C(sp(2))-H and C(sp(3))-H bonds at δ- and ε-positions were effectively activated, thus giving tetrahydroquinolines, benzomorpholines, pyrrolidines, and indolines in moderate to excellent yields by palladium-catalyzed intramolecular C-H amination.