Department of Applied Chemistry, College of Materials and Energy, State Key Laboratory for Conservation and Utilization of Subtropical Agro-bioresources, South China Agricultural University, Guangzhou 510642, China.
Org Biomol Chem. 2019 Aug 28;17(34):7854-7857. doi: 10.1039/c9ob01403a.
A copper-catalyzed DTBP oxidative dual C-H sulfurization has been developed for the direct thiocarbamation of imidazopyridines using a combination of elemental sulfur and formamides as carbamothioyl surrogates. NBS (bromo succinimide) was found to promote the thiocarbamation in good yields. This dual C-H sulfurization strategy enables access to a wide range of carbamothioyl imidazoheterocycles without the use of highly toxic phosgene.
发展了一种铜催化的 DTBP 氧化双 C-H 硫代反应,使用元素硫和甲酰胺作为碳氨硫酰取代基,可直接将咪唑并吡啶硫代氨基甲酰化。发现 NBS(溴代丁二酰亚胺)可以促进硫代氨基甲酰化反应,获得较高产率。这种双 C-H 硫代策略可以在不使用高毒性光气的情况下,获得广泛的碳氨硫酰咪唑杂环化合物。