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固体光气“一锅法”合成卡莫氟

Synthesis of carmofur using triphosgene in one-pot process

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【作者】 张庆伟叶发青郭平刘剑敏

【Author】 ZHANG Qing-wei,YE Fa-qing,GUO Ping,LIU Jian-min(School of Pharmacy,Wenzhou Medical College,Wenzhou 325035,China)

【机构】 温州医学院药学院

【摘要】 以5-氟尿嘧啶、正己胺为原料,用固体光气"一锅法"合成标题化合物,并对反应条件进行初步摸索,即:以吡啶作溶剂、催化剂,原料物质的量比n(固体光气):n(5-FU)=1.2,反应温度50℃,反应时间2h,反应收率可达92.7%。与其他方法相比,该方法操作过程简便、对环境友好、产率较高。

【Abstract】 Carmofur was obtained by the one-pot method based on the reaction of 5-fluorouracil with n-hexylamine using triphosgene as the acylating agent.The technological conditions of synthesis were preliminary explored.The optimum reaction conditions were obtained as follows:pyridine was used as the solvent and catalyst,the ratio of n(triphosgene):n(5-fluorouracil) was equal to 1.2,the reaction temperature was 50 ℃,and the reaction time was 2 h,with the product yield reaching 92.7%.

【关键词】 卡莫氟固体光气一锅法
【Key words】 carmofurtriphosgeneone-pot process
  • 【分类号】TQ463.53
  • 【被引频次】6
  • 【下载频次】338
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