Tanwar Dinesh Kumar, Ratan Anjali, Gill Manjinder Singh
Department of Pharmaceutical Technology (Process Chemistry), National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, Punjab-160062, India.
Org Biomol Chem. 2017 Jun 14;15(23):4992-4999. doi: 10.1039/c7ob00872d.
A novel and simple approach to the synthesis of sulfonylureas has been reported. It involved the reaction of various amines with diphenyl carbonate to yield the corresponding carbamates, which subsequently reacted with different sulphonamides to produce different sulfonylureas in excellent yields. The first reaction of diphenyl carbonate with amines was carried out in aqueous : organic (HO : THF, 90 : 10) medium at room temperature to produce carbamates that paved a straightforward route to sulfonylureas after reaction with sulfonamides. The above process avoided traditional multistep protocols and the use of hazardous, irritant, toxic and moisture sensitive reagents such as phosgene, isocyanates and/or chloroformates.
据报道，一种新颖且简单的合成磺酰脲类化合物的方法。该方法涉及各种胺与碳酸二苯酯反应生成相应的氨基甲酸酯，随后这些氨基甲酸酯与不同的磺酰胺反应，以优异的产率生成不同的磺酰脲类化合物。碳酸二苯酯与胺的第一步反应在水相：有机相（HO：THF，90：10）介质中于室温下进行，生成氨基甲酸酯，该氨基甲酸酯与磺酰胺反应后为磺酰脲类化合物提供了一条直接的合成路线。上述过程避免了传统的多步操作以及使用诸如光气、异氰酸酯和/或氯甲酸酯等危险、刺激性、有毒和对水分敏感的试剂。
