Preparation processes of bambuterol hydrochloride and intermediate thereof

Abstract

The invention relates to preparation processes of bambuterol hydrochloride and an intermediate thereof. The bambuterol hydrochloride is synthesized by taking 3,5-dihydroxyacetophenone as a starting raw material and undergoing esterifying, brominating, reducing, condensing and salting reactions. Compared with other processes, the process has the advantages that: the technical problems of industrial production are solved, each step of reaction is simple, and conditions are mild; and the process is a preparation process with the lowest cost at present, and is successfully applied to industrial production.

Description

technical field [0001] The invention belongs to the field of organic chemistry, and specifically uses 3,5-dihydroxyacetophenone as a starting material to synthesize high-purity bambuterol hydrochloride and its components through 5 steps of esterification→bromination→reduction→condensation→salification Intermediate preparation process. Background technique [0002] Bambuterol hydrochloride is a long-acting beta 2 receptor agonists. The scientific name of bambuterol hydrochloride is 1-[bis-(3′,5′-N,N-dimethylcarbamoyloxy)phenyl]-2-N-tert-butylaminoethanol hydrochloride, and its structural formula is : [0003] [0004] The drug is a new generation of bronchodilator developed by Swiss company Astra in 1989. It is used for the treatment of bronchial asthma and is one of the main drugs for the treatment of asthma, emphysema and bronchitis. Babuterol is a dicarbamate prodrug of terbutaline, with strong lipophilicity, it can be preferentially distributed in the lung tissue a...

AI Technical Summary

Problems solved by technology

[0007] The technical problem to be solved in the present invention is to overcome the technical difficulties that the prior art cannot be used for industrialized production, and to provide a preparation of bambuterol hydrochloride and its intermediates The process, each step of the process is simple and easy to react, and the conditions are mild, which solves the technical difficulties of industrial production. Babuterol hydrochloride has high purity, high yield and low cost, and has been successfully applied in industrial production