固体光气“一锅法”合成卡莫氟

Synthesis of carmofur using triphosgene in one-pot process

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。

Carmofur was obtained by the one-pot method based on the reaction of 5-fluoreuracil 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 %.