The Study On New Synthetic Technology Of Eprosartan

AngiotensionⅡreceptor （AT1） antagonist, which was developed last years, are aseries of medicines with special pharmacological action and excellent curative effectfor cardiovascular diseases such as hypertension, heart failure, and kidney failure, etc.They are the preferred clinical drug that are recommended by WHO （the World HealthOrganization） for hypertension.The mechanisms and the development of angiotension （Ⅱ） receptor （AT1）antagonist were briefly described in this paper. The pharmacological characters andclinical usages of angiotension （Ⅱ） receptor （AT1） antagonist have summarized indetail, A Cost Efficient Synthesis of Eprosartan, which were different from the existingChinese patent, the American patent and the literatures, was designed after carefulresearch on the synthesis of Eprosartan.Based on the domestic and foreign literatures, synthesis route were designed toprovide take Thiophene-2-carboxaldehyde as the raw material, synthesized 3-（2-thiophene） propanoic acid ethyl ester in 97.6％, higher than the value of literature, theseparation operation was simplified. It was better for the industrial appliance; A newroute to synthesis 2-n-butyl-1-[（4-carbonmethoxyphenyl） methyl]imidazole-5-aldehyde, which begun with cheaper materials, was designed. Severalfactors including the catalyst, solvent, reaction time, temperature, the ratio and thesequence of start materials, etc were investigated to optimize the Knoevenagel condensation reation.The structures of the goal compound and the important intermediate compoundswere confirmed by IR, ¹H NMR, ¹³C NMR, UV and melting point.