State Key Laboratory of Functions and Applications of Medicinal Plants, School of Pharmacy, Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education) , Guizhou Medical University , Guiyang 550004 , P. R. China.
State Key Laboratory of Applied Organic Chemistry and College of Chemistry & Chemical Engineering , Lanzhou University , Lanzhou 730000 , P. R. China.
J Org Chem. 2019 Jun 21;84(12):8168-8176. doi: 10.1021/acs.joc.9b01142. Epub 2019 Jun 13.
An organocatalytic asymmetric α-sulfenylation of 2-substituted indolin-3-ones with N-(alkylthio or arylthio)succinimides has been developed for the first time using Cinchona-derived squaramide as the catalyst. Various chiral 2,2-disubstituted indole-3-ones with S- and N-containing heteroquaternary carbon stereocenters were obtained with up to 98% yield and 99% ee.
首次使用金鸡纳衍生的双噁唑啉作为催化剂，发展了一种手性有机催化的 2-取代吲哚啉-3-酮的不对称α-亚磺酰化反应，与 N-（烷基硫代或芳基硫代）琥珀酰亚胺反应。各种手性 2,2-二取代的吲哚-3-酮，具有 S 和 N 杂四元碳手性中心，产率高达 98%，对映选择性高达 99%。
