Wang Wenting, Zhao Lin, Wu Hui, He Youqing, Wu Ge
School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China.
State Key Laboratory of Structural Chemistry, Fujian Institute of Research on the Structure of Matter, Chinese Academy of Sciences, Fuzhou, Fujian 350002, China.
Org Lett. 2023 Oct 6;25(39):7078-7082. doi: 10.1021/acs.orglett.3c02329. Epub 2023 Sep 21.
A metal-free oxidative trideuteromethylthiolation of alkenes with CDSSONa using NFSI as an oxidant has been developed. The aminotrideuteromethylthiolation of a three-component reaction could be easily achieved in the presence of a cobalt catalyst. The divergent trideuteromethylthiolation of alkenes, readily available trideuteromethylthiolation reagent, and versatile synthetic strategy allow for late-stage modification of drug molecules.
已经开发出一种使用NFSI作为氧化剂，将烯烃与CDSSONa进行无金属氧化三氘甲基硫醇化反应的方法。在钴催化剂存在下，可以轻松实现三组分反应的氨基三氘甲基硫醇化。烯烃的发散性三氘甲基硫醇化、易于获得的三氘甲基硫醇化试剂以及通用的合成策略使得药物分子的后期修饰成为可能。
