洛度沙胺氨丁三醇的合成

Synthesis of lodoxamide tromethamine

目的合成新型抗过敏剂洛度沙胺氨丁三醇。方法以 3,5 二硝基 4 氯苯甲酸为起始原料 ,经与SOCl2 作用生成酰氯 ,氨解、脱水、还原反应得到 3,5 二氨基 4 氯苯腈。在三乙胺作用下 ,与草酰氯单乙酯发生酰化反应 ,再经水解得洛度沙胺 ,最后经成盐得洛度沙胺氨丁三醇。结果洛度沙胺氨丁三醇总收率为 2 5 5 % ,其结构经1H NMR、13 C NMR确证。

Objective To synthesize lodoxamide tromethamine which is a new anti-allergic drug.Methods It was synthesized from 3,5-dinitro-4-chlorobenzoic acid in seven steps.Results Lodoxamide tromethamine was synthesized in 25.5% overall yield,and its structure was confirmed by 1H-NMR and 13C-NMR.Conclusions The process of preparing lodoxamide tromethamine is suitable for production on an industrial scale.