Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 60, Issue 18, Pages 9947-9952Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202101076
Keywords
asymmetric trifluorofluoroalkylation; late-stage fluoroalkylation; nickel; reductive cross-coupling
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Funding
- Strategic Priority Research Program of the Chinese Academy of Sciences [XDB20000000]
- National Science Foundation of China [21772187, 21871173, 21971228]
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A nickel-catalyzed asymmetric trifluoroalkylation of aryl iodides was described for the first time, demonstrating high efficiency, mild conditions, and excellent functional group tolerance, especially for substrates containing diverse pharmaceutical and bioactive molecules moieties. This strategy provided an efficient and facile way for diversity-oriented synthesis of chiral trifluoromethylated alkanes.
The trifluoromethyl group represents one of the most functional and widely used fluoroalkyl groups in drug design and screening, while the drug candidates containing chiral trifluoromethyl-bearing carbons are still few due to the lack of efficient methods for the asymmetric introduction of trifluoromethyl group into organic molecules. Herein, we described a nickel-catalyzed asymmetric trifluoroalkylation of aryl iodides, for the first time, by utilizing reductive cross-coupling in enantioselective fluoroalkylation. This novel method has demonstrated high efficiency, mild conditions, and excellent functional group tolerance, especially for substrates containing diverse pharmaceutical and bioactive molecules moieties. This strategy provided an efficient and facile way for diversity-oriented synthesis of chiral trifluoromethylated alkanes.
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