Nickel‐Catalyzed Cross‐Coupling of Functionalized Difluoromethyl Bromides and Chlorides with Aryl Boronic Acids: A General Method for Difluoroalkylated Arenes |
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| Authors: | Yu‐Lan Xiao Wen‐Hao Guo Guo‐Zhen He Qiang Pan Prof. Dr. Xingang Zhang |
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| Affiliation: | Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Lu, Shanghai 200032 (China) |
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| Abstract: | Transition‐metal‐catalyzed difluoroalkylation of aromatics remains challenging despite the importance of difluoroalkylated arenes in medicinal chemistry. Herein, the first successful example of nickel‐catalyzed difluoroalkylation of aryl boronic acids is described. The reaction allows access to a variety of functionalized difluoromethyl bromides and chlorides, and paves the way to highly cost‐efficient synthesis of a wide range of difluoroalkylated arenes. The notable features of this protocol are its high generality, excellent functional‐group compatibility, low‐cost nickel‐catalyst, and practicality for gram‐scale production, thus providing a facile method for applications in drug discovery and development. |
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| Keywords: | boronic acids cross coupling fluorine nickel synthetic methods |
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