Natural Products Research Center, Chengdu Institution of Biology, Chinese Academy of Science, Chengdu 610041, Sichuan, China.
J Org Chem. 2023 Apr 7;88(7):4581-4591. doi: 10.1021/acs.joc.3c00042. Epub 2023 Mar 16.
The sulfinamidines as aza analogues of sulfinamides received limited attention from both organic chemists and pharmaceutical chemists. Herein, we present a tandem oxidative/nucleophilic substitution approach for the synthesis of sulfinamidines in high yield (up to 98%). This cascade reaction method is enabled by N-bromosuccinimide (NBS) as an oxidant and diverse readily available amines as nucleophiles without any additives or catalysts. Notably, this method is highly time-economical, safe to operate, and easy to scale up and has excellent functional group compatibility.
亚磺酰胺的氮类似物——磺胺亚胺,受到有机化学家和药物化学家的关注有限。在此,我们提出了一种串联氧化/亲核取代方法,可高产率(高达 98%)合成磺胺亚胺。该级联反应方法以 N-溴代丁二酰亚胺(NBS)作为氧化剂,各种易得的胺作为亲核试剂,无需任何添加剂或催化剂。值得注意的是,该方法具有高度的时间经济性、操作安全性、易于放大和对功能基团具有良好的兼容性。