Transition metal-free oxidative ortho-acylation of phenols with N-heteroarylmethanes via double C–H activation

Abstract

The direct oxidative acylation of phenols with N-heteroarylmethanes via sp³C–H and sp²C–H double activation was achieved under transition metal-free reaction conditions. This transformation proceeds in a facile I₂/DMSO/O₂ system regio-selectively to produce valuable (2-hydroxyphenyl)arylmethanones from easily available starting materials in moderate to good yields. A plausible mechanism was proposed.