Metal‐Free Regioselective Oxidative C−H Trifluoromethylation of Imidazothiazoles and Their Antitubercular Activity

Abstract

AbstractHere we report a metal‐free direct C−H trifluoromethylation of the imidazothiazoles 7(a–ad) using sodium triflouromethanesulfinate (Langlois’ reagent) and tert‐butyl hydroperoxide (TBHP) as an oxidant. The control studies show that the protocol follows the radical reaction pathway and provides excellent yields of trifluoromethylated products 9(a–ad) with broad substrate scope and regioselective operation. Moreover, the newly synthesized compounds exhibit promising antimycobacterial activity.