Guangdong Key Laboratory of Chiral Molecule and Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Henan Engineering Research Center of Funiu Mountain's Medical Resources Utilization and Molecular Medicine, School of Medical Sciences, Pingdingshan University, Pingdingshan 467000, China.
Org Biomol Chem. 2021 Sep 29;19(37):8030-8034. doi: 10.1039/d1ob01422f.
A series of -chlorosulfurization products bearing difluoromethyl substituents were synthesized in high to excellent yields directly from -toluenesulfonyl difluorodiazoethane (TsCFCHN), disulfides and PhICl without any catalysts or additives. The mild reaction conditions and high functional group compatibility indicated the utility and sustainability of the method. In addition, the -chlorosulfurization products could be efficiently converted to sulfur-containing and aryl substituted difluoromethyl derivatives by a feasible multi-component operation.
直接从 - 对甲苯磺酰基二氟重氮乙烷 (TsCFCHN)、二硫化物和 PhICl 出发,无需任何催化剂或添加剂,就可以高产率、高收率地合成了一系列带有二氟甲基取代基的 - 氯磺化产物。温和的反应条件和高官能团兼容性表明了该方法的实用性和可持续性。此外,- 氯磺化产物可以通过可行的多组分操作有效地转化为含硫和芳基取代的二氟甲基衍生物。