Institute of Organic Chemistry & MOE Key Laboratory of Bioinorganic and Synthetic Chemistry, School of Chemistry, Sun Yat-Sen University, Guangzhou 510275, PR China.
Org Lett. 2020 Oct 2;22(19):7581-7587. doi: 10.1021/acs.orglett.0c02784. Epub 2020 Sep 23.
Thio- and halodifluoromethylated compounds are an important class of compounds in medicinal chemistry and organic synthesis. Herein, we report a facile method for the construction of these compounds via chalcogenide-catalyzed intermolecular electrophilic thio- and halofunctionalization of -difluoroalkenes. Simple treatment of -difluoroalkenes with electrophilic sulfur/halogen reagents and various - or -nucleophiles affords diverse multifunctionalized thio- and halodifluoromethylated compounds. This reaction features a relatively broad substrate scope, good functional group tolerance, and mild reaction conditions.
硫代和卤代二氟甲基化合物是药物化学和有机合成中一类重要的化合物。在此，我们报告了一种通过硫代和卤代亲电官能团化二氟烯烃的方法来构建这些化合物的简便方法。简单地将二氟烯烃与亲电硫/卤试剂和各种 - 或 - 亲核试剂处理，可得到多种多功能化的硫代和卤代二氟甲基化合物。该反应具有较广泛的底物范围、良好的官能团耐受性和温和的反应条件。
