Organocatalytic Asymmetric Cascade Aerobic Oxidation and Semipinacol Rearrangement Reaction: A Visible Light‐Induced Approach to Access Chiral 2,2‐Disubstituted Indolin‐3‐ones

Abstract An enantioselective cascade aerobic oxidation and semipinacol rearrangement reaction of 2‐aryl‐3‐alkyl‐substituted indoles via visible‐light‐driven cooperative organophotoredox and H‐bonding catalysis is reported. The current method provides an expedient and sustainable approach to furnish a variety of valuable chiral 2‐aryl‐2‐alkyl‐substituted indolin‐3‐ones in 64–90 % yield with 58–94 % ee . Preliminary control experiments present important insights into the stereochemistry.