New Non-peptide Angiotensin Ii Receptor Antagonist According To The Synthesis Of Eprosartan

Eprosartan is a new nonpeptide angiotensinâ…¡(Aâ…¡)receptor angtagonist,which was developed by Smithkline Beecham Co.for the management of hypertension in 1997.In this paper,the mechanism and adverse reactions of antihypertensive agents were summarized.At the same time,the developement background and advancement of Aâ…¡receptor angtagonists were described concisely,and the pharmacological characters of Eprosartan were introduced systematically.Furthermore,the synthetic process of eprosartan was particularly studied.According to the reported literatures and domestic chemical materials,one of the synthetic routes was chosen.With p-xylene,thiophene and valeronitrile as the starting materials, Eprosartan(1)was synthesized successfully via convergent synthesis through eighteen steps.The total yield is 12.1%.The melting point of target compound was consentaneously compared with the literature reported and the structure was identified by ~1H-NMR and MS.In this paper,some synthetic routes of 2-butyl-4(5)-formlimidazole(2)were studied and a new synthetic route was designed to get the target compound.With valeronitrile as the starting material,the target compound(2)was synthesized through seven steps.This procedure has the advantage of convenient operations and mild conditions.