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(sp2)H and C(sp3)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. Remote access: The first application of an oxalyl amide to direct CH functionalizations at remote positions is reported. The results show both C(sp2)H and C(sp3)H bonds at δ‐ and ε‐positions are effectively activated, thus giving tetrahydroquinolines, benzomorpholines, pyrrolidines, and indolines in moderate to excellent yields by palladium‐catalyzed intramolecular CH amination.