Copper-Catalyzed Thiolation Annulations of 1,4-Dihalides with Sulfides Leading to 2-Trifluoromethyl Benzothiophenes and Benzothiazoles

Copper-catalyzed double thiolation reaction of 1.4-dihildes with sulfides has been developed for selectively synthesizing 2-trifluoromethyl benzothmphenes and benzothitizoles In the presence of CuI, a variety of 2-halo-1-(2-haloanyl)-3.3.3-trifluoropropylenes smoothily underwent the thiolation annulation with Na2S to afford 2-trifluoromethyl benzothiophenes in moderate to good yields Moreover. the conditions are compatible with N-(2-haloaryl)trifluoroacetimidoyl chlorides in the presence of NaHS and K3PO: leading to 2-trifluoromethyl benzothiazoles