Laboratory of Organic Chemistry, Wageningen University, Stippeneng 4, 6708 WE Wageningen, The Netherlands.
School of Pharmaceutical Science and Technology, Tianjin University, 92 Weijin Road, Tianjin 300072, China.
Org Lett. 2023 Feb 10;25(5):788-793. doi: 10.1021/acs.orglett.2c04292. Epub 2023 Jan 31.
Sulfonamides have many important biological applications, yet their synthesis often involves long reaction times under dry and non-ambient conditions. Here we report the synthesis of a large range of sulfonamides at room temperature using 4-nitrophenyl benzylsulfonate as a starting material. Sulfonamides were prepared from a wide range of aliphatic, linear, and cyclic amines, anilines, and -methylanilines. The yields and reaction times observed here were comparable to or better than those reported previously, establishing sulfur-phenolate exchange as a viable alternative.
磺胺类药物有许多重要的生物学应用，但它们的合成通常需要在干燥和非环境条件下进行长时间的反应。在这里，我们报告了使用 4-硝基苯芐基磺酸酯作为起始原料，在室温下合成一系列磺胺类药物的方法。磺胺类药物可以由各种脂肪族、线性和环状胺、苯胺和 -甲基苯胺制备。这里观察到的产率和反应时间与以前报道的相当或更好，这证明了硫酚交换是一种可行的替代方法。
