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Novel salbutamol drug salt-salbutamol formate and preparation method thereof

A kind of technology of albuterol and formic acid, which is applied in the new albuterol pharmaceutical salt-salbutamol formate and the preparation field thereof, and can solve the problems such as no reports of albuterol formate.

Inactive Publication Date: 2018-05-01
HENAN UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Have not seen any reports about albuterol formate

Method used

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  • Novel salbutamol drug salt-salbutamol formate and preparation method thereof
  • Novel salbutamol drug salt-salbutamol formate and preparation method thereof
  • Novel salbutamol drug salt-salbutamol formate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Add the methanol solution containing 0.46g of formic acid dropwise to the methanol solution containing 2.40g of the salbutamol raw material under magnetic stirring. After the dropwise addition is complete, continue the magnetic stirring reaction for 4h, then pour the reaction solution into a 100ml beaker. The solvent was naturally evaporated, and when a large amount of crystals were formed, the crystals were recovered by filtration, and then recrystallized twice with ethanol, and the yield was calculated after vacuum drying at 65°C for 24 hours, and the yield was 70%.

Embodiment 2

[0025] Add the methanol solution containing 0.23g of formic acid dropwise to the methanol solution containing 1.20g of salbutamol raw material under magnetic stirring. After the dropwise addition is complete, continue the magnetic stirring reaction for 3h, then pour the reaction solution into a 100ml beaker, and The solvent was naturally evaporated, and when a large amount of crystals were formed, the crystals were recovered by filtration, and then recrystallized twice with ethanol, and the yield was calculated after vacuum drying at 65°C for 24 hours, and the yield was 68%.

Embodiment 3

[0027] Add the ethanol solution containing 0.92g of formic acid dropwise to the ethanol solution containing 4.80g of salbutamol raw material under magnetic stirring, after the dropwise addition is complete, continue the magnetic stirring reaction for 4h, then pour the reaction solution into a 100ml beaker, and The solvent was naturally evaporated, and when a large amount of crystals were formed, the crystals were recovered by filtration, and then recrystallized twice with ethanol, and the yield was calculated after vacuum drying at 65°C for 24 hours, and the yield was 64%.

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Abstract

The invention relates to novel salbutamol drug salt-salbutamol formate and a preparation method thereof. The preparation method comprises the following steps: taking salbutamol and formate as raw materials; dropwise adding an alcoholic solution of formate into an alcoholic solution containing salbutamol in a ratio of (1 to 0) to (1 to 2.0), and then, performing stirring for 3 to 4h; performing natural volatilization of a solvent; performing crystallization, and then, performing filtration and crystal recovery; and performing recrystallization by utilizing an alcohol solvent so as to obtain high-purity salbutamol formate of which the yield is greater than 70%. The salbutamol formate product has good crystallinity and thermal stability and has higher solubility than salbutamol in an aqueoussolution.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a new salbutamol pharmaceutical salt-salbutamol formate and a preparation method thereof. Background technique [0002] The chemical name of albuterol is 1-(4-hydroxy-3-hydroxymethylphenyl)-2-(tert-butylamino)ethanol, also known as Kechuanning, which is a selective β2 receptor agonist for the treatment of wheezing Diseases such as bronchitis. Because the solubility is small, and a single salbutamol drug will have some side effects on human health, the method of salbutamol is often used to improve the performance of the drug. Most of it exists in the form of sulfate and hydrochloride on the market to improve its solubility and efficacy. [0003] Currently, there are not many types of salbutamol salts on the market, so further exploration and research on salbutamol salt formation is still necessary. [0004] Also do not see any report about albuterol formate at present. [000...

Claims

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Application Information

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IPC IPC(8): C07C213/08C07C215/60C07C51/41C07C53/06A61P11/00
CPCC07C51/412C07C53/06C07C213/08C07C215/60
Inventor 刘文举赵培侠和萌林申艳敏赵俊廷朱春山刘广宇孙晨
Owner HENAN UNIVERSITY OF TECHNOLOGY
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