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Cu(II)-catalyzed one-pot synthesis of fully substituted dihydrothiophenes and thiophenes from thioamides and enynones
Authors:Min Wen  Pei-Pei Sun  Xiaoyan Luo  Wei-Ping Deng
Institution:Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai, 200237, China
Abstract:A facile and direct synthetic method was developed for the construction of fully substituted dihydrothiophenes, which via a copper-catalyzed Michael addition/intramolecular cyclization/protonation cascade reaction of readily available thioamides with enynones under air atmosphere. This approach provides 2,3-dihydrothiophenes with up to 92% yield in a one-pot process. In addition, several fully substituted thiophenes could also be synthesized by changing the substituents of thioamides.
Keywords:Cu(II)-Catalyzed  Dihydrothiophenes  Thiophenes  Thioamides  Enynones
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