Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 53, Issue 37, Pages 9909-9913Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201405653
Keywords
boronic acids; cross coupling; fluorine; nickel; synthetic methods
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Funding
- National Basic Research Program of China (973 Program) [2012CB821600]
- NSFC [21172242, 21332010]
- SIOC
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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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