二丙酸咪唑苯脲的合成工艺改进  

Improved Synthesis of Imidocarb Dipropionate

作　　者：崔新强 孔祥雨 张彬 李新志 刘文涛 于治见 杨利 CUI Xin-qiang;KONG Xiang-yu;ZHANG Bin;LI Xin-zhi;LIU Wen-tao;YU Zhi-jian;YANG Li(Shandong Provincial Key Laboratory of Chemical Drugs,Shandong Academy of Pharmaceutical Science,Jinan 250101,China)

机构地区：[1]山东省药学科学院山东省化药重点实验室,山东济南250101

出　　处：《食品与药品》2020年第5期383-385,共3页Food and Drug

摘　　要：目的对二丙酸咪唑苯脲的合成工艺进行改进。方法以间硝基苯甲腈为原料,经与乙二胺环化,硝基还原,与尿素缩合制得咪唑苯脲粗品,再与丙酸成盐制得二丙酸咪唑苯脲。结果合成的目标产物收率为69.7%,纯度为99.3%。所得产物经熔点、质谱(MS)和核磁共振氢谱(1H-NMR)等方法确证。结论改进后的工艺减少了废弃物的产生,实现了绿色化生产,收率高,操作简便,适合工业化生产。Objective To improve the synthesis process of imidocarb dihydrochloride.Methods Using 3-nitrobenzonitrile as the starting material,imidocarb dipropionate was prepared by cyclization with ethylenediamine,reduction of nitro group,condensation with urea and salt formation.Results The purity of the target product was 99.3%,and the overall yield reached 69.7%.The structure of imidocarb dihydrochloride was confirmed by melting point determination,MS and 1H-NMR.Conclusion The improved process can reduce the generation of waste and realize green production,increase yield,simplify operation and is suitable for industrial production.

关 键 词：梨形虫病 咪唑苯脲 工艺改进 

分 类 号：R914.5[医药卫生—药物化学]