Method for preparing anti-platelet aggregation compounds

Abstract

The invention belongs to the technical field of pharmaceutical chemistry, in particular to a new method for preparing anti-platelet aggregation compounds with a structure shown in a general formula I. In the preparation route, cheap and readily available initiative materials, namely methyl alpha-bromo-2-chlorophenylacetate and thiophene-2-ethylamine, replace clopidogrel in the conventional document. Concretely, the methyl alpha-bromo-2-chlorophenylacetate is reacted with the thiophene-2-ethylamine, replace clopidogrel under the catalysis of an acid-catcher to generate an intermediate II; the intermediate II is reacted with hydrazine hydrate, acetone or 3-pentanone to generate an intermediate III; and the intermediate III undergoes cyclization to generate the compounds in the formula I. The method has the advantages of mild reaction conditions, simple and safe operating process, and easy industrial production; and the product has stable quality, high purity and high yield; compared with that of the synthetic process provided by the conventional document, the production cost is greatly reduced; and in the formula I, R refers to methyl or ethyl.

Description

technical field The invention belongs to the technical field of chemical pharmacy, in particular to a synthesis method of a class of anti-platelet aggregation compounds, in particular to an industrial production method of the anti-platelet aggregation compounds. Background technique Thrombosis can lead to acute myocardial infarction, stroke, pulmonary embolism and other diseases of the heart, brain, and pulmonary circulation, threatening human health and life, and is also a common complication in surgery and a factor of reocclusion after interventional angioplasty. Although thrombolytic therapy, interventional therapy and even surgical treatment carried out in recent years have made remarkable progress in the treatment of acute myocardial infarction and cerebral infarction, the success rate of patient rescue has been greatly improved, and the quality of life has also been significantly improved, but cardiovascular and cerebrovascular After all, the disability rate is as high...

AI Technical Summary

Problems solved by technology

Aiming at the deficiencies of the prior art, the present invention provides a method for preparing the compound of formula I suitable for large-scale industrial production. The purpose of the present invention is to overcome the disadvantage of high raw material prices in the existing synthesis method, and to select low-cost and easy-to-obtain compounds while ensuring product quality. Raw materials, thereby reducing production costs, suitable for large-scale industrial production

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