Nitroarenes are used as the coupling partners in the preparation of sulfonamides via the insertion of sulfur dioxide. A three-component reaction of arylboronic acids, nitroarenes, and potassium metabisulfite under copper catalysis proceeds smoothly, giving rise to a range of sulfonamides in good to excellent yields with broad substrate scope. Various functional groups including hydroxyl, cyano, amino
硝基
芳烃通过插入
二氧化硫用作磺酰胺的偶联伙伴。在
铜催化下,芳基
硼酸,硝基
芳烃和偏
亚硫酸氢钾的三组分反应平稳进行,从而产生了一系列磺
酰胺类化合物,具有良好的收率和优异的收率,具有广泛的底物范围。包括羟基,
氰基,
氨基和羰基在内的各种官能团都是可以耐受的。提出了一个合理的机理,表明芳基亚
磺酸盐是中间体,硝基
芳烃和芳基亚
磺酸盐的
铜辅助相互作用是关键步骤。该方法还扩展到当前市售药物(
氟他胺)的后期修饰。