奥美沙坦关键中间体的新合成方法

摘要

Objective To synthesize the important intermediates of Olmesartan.Methods 2-propyl-1H-imidazole-4,5-dicarboxylic acid diethyl ester was synthesized using tartaric acid,an easily available,inexpensive and renewable substrate,as starting material via nitration,cyclization,esterifcation.Results The technics was improved and toxic material was replaced.The overall yield was 70%.Conclusion The improved method is of high yield,more practical,facile and suitable for industry.%目的 合成抗高血压新药奥美沙坦的关键中间体2-丙基-1H-咪唑-4,5-二羧酸二乙酯. 方法以价廉易得、可再生的酒石酸为起始原料,经混酸硝化后与醛氨溶液缩合,再经酯化制得.结果 取代了文献中有毒的原料,改进了合成工艺,总收率提高到70%.结论 以酒石酸为起始原料的改进后的合成方法收率提高,反应条件温和,适合工业化生产.