Guangdong Provincial Key Laboratory of Chiral Molecules and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
J Org Chem. 2021 Feb 5;86(3):3041-3048. doi: 10.1021/acs.joc.0c02511. Epub 2021 Jan 27.
An enantioselective Michael addition between -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.
一种对映选择性迈克尔加成反应，在 -2,2,2-三氟乙基靛红亚胺和亚乙基磺酰氟之间发生。这种方法提供了一种简便的策略，可以获得一系列结构多样的靛红衍生的 α-（三氟甲基）亚胺衍生物，具有优异的产率和对映选择性。α-（三氟甲基）胺和磺酰氟基团的有趣组合为药物发现提供了有价值的候选物。
