Copper(II) mediated C–H methylthiolation of 2-phenyl pyridines with dimethyl sulfoxide using an amino acid ligand |
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| Authors: | Yan Xiao Shuo Wang Jianyu Liu Hui Zhang Yongnan Xu |
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| Institution: | 1. Department of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Wenhua Road 103#, Shenyang, Liaoning 110016, China;2. Key Laboratory of Structure-based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Wenhua Road 103#, Shenyang, Liaoning 110016, China |
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| Abstract: | A novel protocol for the C–H methylthiolation of 2-phenyl pyridines using DMSO as the methylthio source and an amino acid ligand is described. This simple procedure requires neither an oxidant nor additional solvent. The developed protocol tolerates a wide range of functional groups including methyl, methoxy, fluoro, chloro, and in particular the formyl group. This new strategy is highly regioselective and provides aryl methyl sulfides from 2-phenyl pyridines in moderate to good yields. |
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| Keywords: | C–H methylthiolation Aryl methyl sulfide Amino acid Dimethyl sulfoxide |
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