Highly Enantioselective Addition of N-2,2,2-Trifluoroethylisatin Ketimines to Ethylene Sulfonyl Fluoride.


Chen J(1), Zhu DY(1), Zhang XJ(1), Yan M(1).
Author information:
(1)Guangdong Provincial Key Laboratory of Chiral Molecules and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.


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 α-(trifluoromethyl)imine derivatives with excellent yields and enantioselectivities. The intriguing combination of α-(trifluoromethyl)amine and sulfonyl fluoride groups leads to the valuable candidates for the drug discovery.