Preparation method of salbutamol intermediate V hydrochloride

A technology of albuterol and intermediates, applied in the field of preparation of albuterol intermediate V hydrochloride
CN108623486AInactive Publication Date: 2018-10-09CHONGQING CONQUER PHARML
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
CHONGQING CONQUER PHARML
Publication Date
2018-10-09
Estimated Expiration
Not applicable · inactive patent

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Abstract

Salbutamol is a beta receptor stimulant. In the conventional preparation technology of salbutamol, reference listed drug technology is taken as the main research content; in the reference listed drugtechnology, p-Hydroxyacetophenone is taken as an initial material, chloromethylation, esterification, bromination, amination, hydrolysis, and reduction are adopted to prepare salbutamol. According tothe reparation method of salbutamol intermediate V hydrochloride, intermediate IV and N-Benzyl-tert-butylamine are subjected to backflow reaction in reaction solvent ethyl acetate, and filtering and acidifying are carried out so as to realize product extraction into a water layer, hydrolysis and alkalization are carried out at backflow states, extractant ethyl acetate is adopted for extraction, and concentration is carried out so as to obtain a free alkali compound of the intermediate V; and the free alkali is dissolved in an organic solvent, and hydrochloric acid is added dropwise so as to obtain the salbutamol intermediate V hydrochloride.
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Description

technical field

[0001] The invention relates to the field of medicine and chemical industry, in particular to a preparation method of albuterol intermediate V hydrochloride. Background technique

[0002] Salbutamol is a beta-receptor agonist mainly used in the treatment of bronchospasm caused by wheezing bronchitis, bronchial asthma, and emphysema. Due to the frequent occurrence of global respiratory diseases, the consumption of salbutamol also remains high. At present, the preparation process of salbutamol is mainly based on the original research process. The original research process uses p-hydroxyacetophenone as the starting material, and prepares salbutamol through chloromethylation, esterification, bromination, amination, hydrolysis and reduction. The route is as follows:

[0003]

[0004] In the above synthetic route, toluene is used as the reaction solvent in the preparation of intermediate IV from intermediate IV, and benzene, a class I solvent, is introduced, r...

Claims

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