PhI(OAc)2 oxidative C5 halogenation of quinolines using copper halides under mild conditions

Abstract

A concise and efficient protocol for PhI(OAc)₂ oxidation halogenation of quinoline at the C5 position was developed, affording the desired remote C–H activation products in moderate to excellent yields. This reaction proceeds with copper halides as the halogenating reagent to afford the halogenated quinolines and features excellent substrate tolerance, providing a facile pathway for the C5 halogenation of quinoline.