烟拉文的合成工艺改进

Improved synthesis of nicaraven

以烟酸为原料 ,与氯甲酸乙酯反应 ,生成混合酸酐 ,再与 1 ,2 丙二胺反应得到烟拉文粗品 ,通过形成二硝酸盐再碱化的方法得到烟拉文纯品。以 1 ,2 丙二胺计 ,总收率为 3 8 8% ,结构经IR、MS及1H NMR确证 ,该合成工艺简单易行。

Nicaraven was synthesized from nicotinic acid by the reaction with ethyl chlorocarbonate to form a mixed acid anhydrides which reacted with 1,2-propanediamine and then aqueous nitric acid solution,followed by alkalization with saturated sodium carbonate.The overall yield of the improved procedure was 38.8%.The structure of nicaraven was confirmed by IR,MS and 1H-NMR.The process is simple and practical.