摘要
1,3-二氢苯并[c]异噻唑2,2-二氧化物是常见的药物骨架,本文以邻氯氯苄和亚硫酸钠为原料,经亲核取代、酰氯化、酰胺化及偶联环化反应,以55%的总收率和99%的纯度合成了1,3-二氢苯并[c]异噻唑2,2-二氧化物,其结构经~1H NMR,^(13)C NMR和FT-IR确证。
1,3-Dihydrobenzo[ c ]isothiazole 2,2-dioxide is prevalent moiety in many pharmaceuticals. It was synthesized using 1-chloro-2-(chloromethyl)benzene and sodium sulfite as raw materials through nucleophilic substitution, acyl chloride, amidation and coupling cyclization reaction in 55% total yield and up to 99% purity. The structure was confirmed by 1HNMR, 13CNMR and FT-IR.
作者
刘小兵
吴韦
杨云
陈莹莹
毛国梁
LIU Xiao-bing;WU Wei;YANG Yun;CHEN Ying-ying;MAO Guo-liang(Provincial Key Laboratory of Oil&Gas Chemical Technology,College of Chemistry and Chemical Engineering,Northeast Petroleum University,Daqing 163318,China)
出处
《合成化学》
CAS
北大核心
2019年第3期219-221,228,共4页
Chinese Journal of Synthetic Chemistry
基金
国家自然科学基金资助项目(U1362110)
