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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。
OBJECTIVE To synthesize diethyl 2-propyl-1H-imidazole-4,5-dicarboxylate, the key intermediate of anti-hypertensive drug olmesartan. The method is cheap and readily available, renewable tartaric acid as the starting material, after mixed acid nitration and aldehyde ammonia solution condensation, and then obtained by esterification. The results replaced the toxic raw materials in the literature, improved the synthesis process, the total yield increased to 70%. Conclusion The improved synthesis method with tartaric acid as starting material has higher yield, mild reaction conditions and is suitable for industrialized production.