沈阳药科大学学报

2004, (03) 185-186+189

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洛度沙胺氨丁三醇的合成
Synthesis of lodoxamide tromethamine

陈国良,薛建英,单韦,张瑞华
CHEN Guo-liang 1; XUE Jian-ying 1; SHAN Wei 1; ZHANG Rui-hua 2 (1. School of Pharmaceutical Engineering;

摘要(Abstract):

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。结论该合成方法适合工业化大生产
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.

关键词(KeyWords): 洛度沙胺氨丁三醇;合成;抗过敏
lodoxamide tromethamine; synthesis; anti-allergic

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作者(Authors): 陈国良,薛建英,单韦,张瑞华
CHEN Guo-liang 1; XUE Jian-ying 1; SHAN Wei 1; ZHANG Rui-hua 2 (1. School of Pharmaceutical Engineering;

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