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

Abstract

In general, enantioselective C-H functionalization of <i>N</i>-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 <i>para</i> C-H aminoalkylation of <i>N</i>-monosubstituted aniline derivatives with isatin-derived ketimines in the presence of chiral phosphoric acids (CPAs) and offered a practical strategy for <i>para</i> asymmetric C-H functionalization of anilines containing N-H bonds.