Coupling of Heteroaryl Halides with Chlorodifluoroacetamides and Chlorodifluoroacetate by Nickel Catalysis |
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| Authors: | Dawei Zhang Xing Gao Qiao-Qiao Min Dr. Yucheng Gu Dr. Guillaume Berthon Prof. Dr. Xingang Zhang |
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| Affiliation: | 1. Key Laboratory of Organofluorine Chemistry, Center for Excellence in Molecular Synthesis, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences Chinese Academy of Sciences, 345 Lingling Lu, Shanghai, 200032 P. R. China;2. Syngenta Jealott's Hill International Research Centre, Bracknell, RG42 6EY UK;3. Syngenta Japan K.K., 21F, Office Tower X, 1-8-10. Harumi, Chuo, Tokyo, 104-6021 Japan |
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| Abstract: | A nickel-catalyzed cross-coupling of heteroaryl halides with chlorodifluoroacetamides and chlorodifluoroacetate has been developed. The combination of NiCl2 ⋅ DME with 4,4′-diNon-bpy, co-ligand PPh3, and additive LiCl renders the catalytic system efficient for the synthesis of medicinal interest heteroaryldifluoroacetamides. The application of the method leads to short and highly efficient synthesis of biologically active molecules, providing a facile route for applications in medicinal chemistry and agrochemistry. |
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| Keywords: | catalysis chlorodifluoroacetamides heteroaryl halides nickel reductive cross coupling |
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