Journal
JOURNAL OF ORGANIC CHEMISTRY
Volume 86, Issue 3, Pages 3041-3048Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.0c02511
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Funding
- National Natural Science Foundation of China [21772240]
- Guangdong Provincial Key Laboratory of Chiral Molecules and Drug Discovery [2019B030301005]
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An enantioselective Michael addition has been developed for the synthesis of structurally diverse isatin-derived alpha-(trifluoromethyl)imine derivatives with excellent yields and enantioselectivities, which are valuable candidates for drug discovery.
An enantioselective Michael addition between N-2,2,2-trifluoroethylisatin ketimines and ethylene sulfonyl fluoride has been disclosed. This method provides a facile strategy to access a range of structurally diverse isatin-derived alpha-(trifluoromethyl)imine derivatives with excellent yields and enantioselectivities. The intriguing combination of alpha-(trifluoromethyl)amine and sulfonyl fluoride groups leads to the valuable candidates for the drug discovery.
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