C–H chlorination of (hetero)anilines via photo/organo co-catalysis

Abstract

Chlorinated (hetero)anilines are a class of important structural motifs that are widely present in synthetic building blocks and pharmaceuticals. Despite recent advancements, direct aniline chlorination still suffers from ortho/para and mono/poly chlorination selectivity problems. Herein, we disclose a photo-redox and organo co-catalyzed chlorination method for anilines. This method has great substrate generality and excellent mono-chlorination selectivity. Another merit of this method is the late-stage modification of drug molecules, which would be useful in medicinal chemistry.