Highly Chemo‑, Site‑, and Enantioseletive para C–H Aminoalkylation of N‑Monosubstituted Aniline Derivatives Affording 3‑Amino-2-oxindoles

In general, enantioselective C–H functionalization of N-monosubstituted anilines is a highly challenging task owing to the competitive chemoselective N–H bond insertion reactions. In this paper, we reported a direct highly chemo-, site-, and enantioselective para C–H aminoalkylation of N-monosubstituted aniline derivatives with isatin-derived ketimines in the presence of chiral phosphoric acids (CPAs) and offered a practical strategy for para asymmetric C–H functionalization of anilines containing N–H bonds.