药学相关磺酰基-（硫代）脲的机械合成
Mechanosynthesis of pharmaceutically relevant sulfonyl-(thio)ureas.
作者信息
Tan Davin, Štrukil Vjekoslav, Mottillo Cristina, Friščić Tomislav
机构信息
Department of Chemistry and FRQNT Centre for Green Chemistry and Catalysis, McGill University, Montreal, Canada.
出版信息
Chem Commun (Camb). 2014 May 25;50(40):5248-50. doi: 10.1039/c3cc47905f. Epub 2013 Nov 20.
PMID:24256886
Abstract
We demonstrate the first application of mechanochemistry to conduct the synthesis of sulfonyl-(thio)ureas, including known anti-diabetic drugs tolbutamide, chlorpropamide and glibenclamide, in good to excellent isolated yields by either stoichiometric base-assisted or copper-catalysed coupling of sulfonamides and iso(thio)cyanates.
摘要
我们展示了机械化学在磺酰基 -（硫代）脲合成中的首次应用，通过化学计量碱辅助或铜催化的磺酰胺与异（硫代）氰酸酯的偶联反应，以良好至优异的分离产率合成了包括已知抗糖尿病药物甲苯磺丁脲、氯磺丙脲和格列本脲在内的化合物。
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