A general method for site-selective Csp3–S bond formation via cooperative catalysis |
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| Authors: | Yuman Qin Yujie Han Yongzhen Tang Junfa Wei Mingyu Yang |
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| Affiliation: | Key Laboratory of Applied Surface and Colloid Chemistry of MOE, School of Chemistry and Chemical Engineering, Shaanxi Normal University, 620 West Chang''an Ave, Xi''an 710119 China, |
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| Abstract: | Herein, we report a copper-catalysed site-selective thiolation of Csp3–H bonds of aliphatic amines. The method features a broad substrate scope and good functional group compatibility. Primary, secondary, and tertiary C–H bonds can be converted into C–S bonds with a high efficiency. The late-stage modification of biologically active compounds by this method was also demonstrated. Furthermore, the one-pot preparation of pyrrolidine or piperidine compounds via a domino process was achieved.A copper-catalyzed site-selective thiolation of Csp3–H bonds of aliphatic amines was developed. The method features a broad substrate scope and good functional group tolerance. |
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