Easily Accessible Auxiliary for Palladium‐Catalyzed Intramolecular Amination of C(sp<sup>2</sup>)H and C(sp<sup>3</sup>)H Bonds at δ‐ and ε‐Positions

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<jats:title>Abstract</jats:title><jats:p>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<jats:sup>2</jats:sup>)H and C(sp<jats:sup>3</jats:sup>)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.</jats:p>

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