Despite the fact that the direct C-H transformation of various compounds has been established,tertiary anilines remain a big challenge for transition-metal catalyzed ortho-selective aromatic C-H functionalization,partly due to the steric hindrance of tertiary amino groups.1 On the other hand,transformation of C-N bond has become a hot area in organic synthesis over the past years.2 Recently,it is known that the integration of C-H activation and O atom transfer (OAT) has been realized by the utilization of[Cp*RhⅢ]catalyst) Herein,[Cp*RhⅢ]-catalyzed annulation of tertiary aniline N-oxides with alkynes was reported to achieve the challenging ortho C-H functionalization of tertiary anilines via N-O bond acting as a traceless directing group.More significantly,this system represents the first example which integrates C-H activation,oxygen-atom transfer,and N-dealkylative cyclization in one reaction.This unprecedented coupling reaction has allowed the construction of N-alkylindole derivatives in high efficiency with broad substrate scope and good functional group tolerance.