Direct C2-arylation of indoles enabled by photoinduced XAT and Co-mediated desaturation

Abstract

2-Arylindoles are important motifs that serve as key components in a large variety of biologically active molecules and pharmaceuticals. Herein, we report a photoredox/Co-catalysis-enabled regioselective C2-arylation of indoles. This protocol allows for facile construction of a series of 2-arylindoles from structurally varied indoles and various aryl halides, featuring excellent regioselectivity, broad substrate scope, and good reaction efficiency. Mechanistically, the rational combination of photoredox-driven halogen-atom transfer (XAT) and Co-mediated desaturation ensured the success of this newly developed methodology.