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Production technology for synthetizing salbutamol sulphate

A salbutamol sulfate and production process technology, which is applied in the field of synthesizing salbutamol sulfate, can solve the problems of troublesome post-processing, low yield, and many side reactions, and achieve the effects of short reaction steps, easy availability of raw materials, and reduced product cost

Inactive Publication Date: 2015-02-18
扬州市三药制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0024] The purpose of the present invention is to provide a new process for the improved synthesis of albuterol, so as to solve technical defects such as many side reactions, low yield and troublesome post-processing of the existing synthetic process

Method used

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  • Production technology for synthetizing salbutamol sulphate
  • Production technology for synthetizing salbutamol sulphate
  • Production technology for synthetizing salbutamol sulphate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] (1) Preparation of compound 3 (5-bromoacetyl-2-hydroxybenzaldehyde):

[0044] Add 55 grams of anhydrous aluminum chloride to the reaction bottle, stir and add 50 milliliters of anhydrous dichloromethane, 20 milliliters of anhydrous dichloroethane, heat up to 50 ° C, start to drop 23.3 grams of chloroacetyl chloride, dropwise, Start to add 11 grams of salicylaldehyde dropwise. After the dropwise addition, keep the temperature at 50° C. for 20 hours to react. The reaction solution is lowered to room temperature, and slowly added dropwise to the mixed solution of 150 grams of water and 50 milliliters of dichloromethane. Add 20 ml of concentrated hydrochloric acid, stir, separate the organic phase, extract the aqueous phase with 300 ml of dichloromethane × 2, concentrate under reduced pressure at 40-45°C to obtain a yellow solid and a small amount of oil, stir, crystallize and filter under ice-water bath cooling to obtain The light yellow solid was dried to constant weight ...

Embodiment 2

[0056] (1) Preparation of Compound 3:

[0057] Add 110 grams of anhydrous aluminum chloride to the reaction flask, stir and add 100 milliliters of anhydrous dichloromethane, 50 milliliters of anhydrous dichloroethane, heat up to 50 ° C, start to drop 23.3 grams of bromoacetyl chloride, dropwise, Start to add 22 grams of salicylaldehyde dropwise. After the dropwise addition, keep the temperature at 50° C. for 20 hours to react. The reaction solution is lowered to room temperature, and slowly added dropwise to the mixed solution of 300 grams of water and 100 milliliters of dichloromethane. Add 50 ml of concentrated hydrochloric acid, stir, separate the organic phase, extract the aqueous phase with 500 ml of dichloromethane × 2, concentrate under reduced pressure at 40-45°C to obtain a yellow solid and a small amount of oil, stir, crystallize and filter under ice-water bath cooling to obtain Light yellow solid, dried to constant weight to obtain 35.5 g of compound 3.

[0058] (2...

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Abstract

The invention discloses a production technology for synthetizing salbutamol sulphate, and relates to the field of chemical synthesis. The production technology comprises the following steps: firstly, performing an Friedel-crafts acylation reaction on salicylal to obtain a chemical compound 3, performing a substitution reaction of tert-butylamine, protecting dihydroxy by propylidene under the catalysis of concentrated sulfuric acid through the reduction of potassium borohydride or sodium borohydride, then performing extraction for desalting, and generating a hydrolysis reaction under acid conditions to obtain sulphuric acid salbutamol. The production technology disclosed by the invention is easy to control and operate, raw materials are simple and easy to obtain, the total mol yield is as high as 40%, the product purity is as high as 99.5%, and the product cost is low.

Description

technical field [0001] The invention relates to the field of chemical synthesis, in particular to a new method for synthesizing salbutamol sulfate. Background technique [0002] Salbutamol sulfate 1-(4-hydroxy-3-hydroxymethylphenyl)-2-(tert-butylamino)ethanol sulfate is a potent and fast-acting selective b-receptor agonist for asthmatic bronchitis, Respiratory diseases such as bronchospasm in patients with bronchial asthma and emphysema all have a good therapeutic effect. Salbutamol was discovered by British scholars in 1962 and developed by the British Glaxo Company. It was first listed in 1968, registered in my country in 1988, and produced in China in 1975. Although this is an old drug, it still plays an irreplaceable role. In recent years, its sales in the world pharmaceutical market have ranked before the top 20. The formulations of albuterol include tablets, capsules, aerosols and injections. [0003] Due to environmental pollution, the smog weather in our country h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C215/60C07C213/00
Inventor 祝瑞章刘长福徐园陈林谢文杰
Owner 扬州市三药制药有限公司
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