直接二氟甲硫基化与一氟甲硫基化反应研究进展  

Recent Progress on Direct Difluoromethylthiolation and Monofluoromethylthiolation

作　　者：闫强 蒋绿齐 易文斌[1] Yan Qiang;Jiang Lüqi;Yi Wenbin(Chemical Engineering College,Nanjing University of Science and Technology,Nanjing 210094)

机构地区：[1]南京理工大学化工学院,南京210094

出　　处：《有机化学》2020年第1期1-14,共14页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.21476116);中央高校基本科研业务费专项资金(No.30918011314);江苏省自然科学基金(No.BK20141394);江苏省青蓝计划;六大高峰人才资助项目。

摘　　要：含有二氟甲硫基基团(SCF2H)与含有一氟甲硫基基团(SCFH2)的有机化合物具有独特的物理和化学性质,在医药及农药等领域具有潜在的应用价值.这两类化合物的传统制备方法是巯基底物的二氟甲基化与一氟甲基化,但含巯基底物本身种类有限,极大地限制了该类化合物的应用与开发,因此开发新的直接二氟/一氟甲硫基化方法和开拓新型直接二氟/一氟甲硫基化试剂具有重要的意义.综述了直接二氟甲硫基化反应和一氟甲硫基化反应的最新研究进展,并对反应的相关机理进行了论述.Compounds bearing difluoromethylthio(SCF2 H) and monofluoromethylthio(SCFH2) groups are potentially important targets in the pharmaceutical and agrochemical fields due to their unique physical and chemical properties. The traditional methods of synthesizing these two kinds of compounds are difluoromethylation and monofluoromethylation of sulfhydryl substrates. However, the limitation of sulfhydryl substrates also limited the application and development of such compounds. Thus, it is still highly desirable to develop new methods for difluoromethylthiolation and monofluoromethylthiolation as well as new types of difluoromethylthiolation and monofluoromethylthiolation reagents. The recent development of direct difluoromethylthiolation and monofluoromethylthiolation reactions is summarized, and the related mechanism are also discussed.

关 键 词：二氟甲硫基化 一氟甲硫基化 直接法 

分 类 号：O621.25[理学—有机化学]