Modified preparation method for eprosartan

Abstract

The invention discloses a preparation process of improved eprosartan, which using compounds which are showed by formula (1) and formula (2) as raw materials, decompressing and separating water in reflux in solvent which can be boiled with water under the catalysis effect, controlling reflux temperature between 50 DEG C and 100 DEG C, fully reacting to obtain compound which is showed in formula (3), hydrolyzing the compound in formula (3) under the alkali to remove ester group, finally obtaining eprosartan showed in formula (4) after being regulated the pH value of reaction liquor to acidic property. The yield of eprosartan product is greatly increased through the invention, and the purity is excellent, thereby greatly reducing production cost.

Description

technical field The invention relates to a preparation method of Eprosartan and belongs to the field of medicinal chemistry. Background technique Eprosartan (compound of formula (4)), the chemical name is (E)-α-[[2-butyl-1-[(4-carboxyphenyl)methyl]-1hydro-imidazol-5-yl ]-2-thiophenepropionic acid. Eprosartan is an angiotensin II receptor blocker and is the latest generation of antihypertensive drugs. Clinical studies have shown that the drug is effective in reducing systolic blood pressure and diastolic blood pressure in patients with mild, moderate and severe hypertension, and has good safety and tolerance. As a highly effective and selective angiotensin subtype 1 (AT1) receptor antagonist, eprosartan plays an antihypertensive role by blocking the angiotensin II receptor. Patent US5185351 describes its synthesis method and use. US5185351 describes a series of synthetic methods of imidazole compounds, including the synthesis of eprosartan. One of the methods uses the...

AI Technical Summary

Problems solved by technology

This method yield is very low (40%), and cost is higher, is not applicable to the requirement of suitability for industrialized production

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