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

Here 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