- Copper-catalyzed thiolation annulations of 1,4-dihalides with sulfides leading to 2-trifluoromethyl benzothiophenes and benzothiazoles
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Copper-catalyzed double thiolation reaction of 1,4-dihalides with sulfides has been developed for selectively synthesizing 2-trifluoromethyl benzothiophenes and benzothiazoles. In the presence of CuI, a variety of 2-halo-1-(2-haloaryl)-3,3,3-trifluoropropylenes smoothly 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 K3PO4, leading to 2-trifluoromethyl benzothiazoles.
- Li, Chun-Lin,Zhang, Xing-Guo,Tang, Ri-Yuan,Zhong, Ping,Li, Jin-Heng
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supporting information; experimental part
p. 7037 - 7040
(2010/11/17)
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