铜促进8-氨基喹啉导向的芳基酰胺的二甲硫基化反应  

Copper-Promoted Dimethylthiolation of Benzamides under Assistance of 8-Aminoquinoline Group

作　　者：郭圆圆 刘振伟 朱明祥 李琳琳 李敬亚 邹大鹏[1] 吴豫生 吴养洁[1] Guo Yuanyuan;Liu Zhenwei;Zhu Mingxiang;Li Linlin;Li Jingya;Zou Dapeng;Wu Yusheng;Wu Yangjie(College of Chemistiy and Molecular Engineerings Zhengzhou University,Zhengzhou 450052;Tetranov Biopharm,LLC,Zhengzhou 450052)

机构地区：[1]郑州大学化学与分子工程学院,郑州450052 [2]郑州泰基鸿诺医药股份有限公司,郑州450052

出　　处：《有机化学》2020年第3期724-730,共7页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(Nos.21172200.21702191)资助项目.

摘　　要：报道了利用廉价易得的二甲基亚砜作为甲硫基源,实现8-氨基喹啉导向的芳基酰胺的二甲硫基化反应.利用CuSO4·5H2O作为促进剂,以中等到较好的收率高效地合成了一系列含有二甲硫基的芳酰胺衍生物.此外,该反应体系具有反应条件温和、不需要外加其它氧化剂的特点.Cu(Ⅱ)-promoted dimethylthiolation of C(sp2)一H bonds using DMSO as the methylthiolation source with the assista nee of an 8-aminoquinoline directing group have been developed.A number of dimethylthiolated benzamides were efficiently synthesized using CuSO4e5H2O as a promoter in moderate to good yields.In addition,this reaction system features facile conditions and no other oxidant additive was required.

关 键 词：二甲硫基化 二甲基亚砜 8-氨基喹啉 Cu促进 

分 类 号：O621.25[理学—有机化学]