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以邻苯二胺为起始原料,经5步反应合成了富马酸依美斯汀(1).采用加入相转移催化剂的方法,改进了2个关键中间体2-氯-1-(2-乙氧基乙基)苯并咪唑(4)和依美斯汀(5)的合成工艺.反应无需控制水分,中间体4和5的收率分别提高至67.9%和74.9%.产物的结构经IR、1H NMR、13C NMR、质谱、元素分析、差热分析及X射线粉末衍射证实.

参考文献

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