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Method for preparing metoprolol salt

A technology of mixed solvent and acetone, which is applied in the field of metoprolol salt preparation, can solve the problems of complex pH value detection process, difficult removal of impurities, long reaction time, etc., and achieve easy recycling, reduction of three wastes discharge, and simple treatment Effect

Active Publication Date: 2016-11-09
ZHEJIANG YONGTAI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This process has the disadvantages of low yield, long reaction time, difficult removal of impurities, complex pH value detection process, high production cost, and low product quality.

Method used

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  • Method for preparing metoprolol salt
  • Method for preparing metoprolol salt

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] First the mixed system of tartaric acid (0.5mol, 75g), acetone (890g) and water (61.4g) was warmed up and refluxed until tartaric acid was completely dissolved, then under reflux, formula (II) metoprolol (1mol, 267g) Add the mixed solution of acetone (311.5g) dropwise to the solution, after the dropwise addition, keep it warm at 50-65°C for 0.5 hours, cool to 0-5°C, stir and crystallize for 1 hour, after the crystallization , suction filtration, drying to obtain formula (I) metoprolol salt 307.22g, productive rate 89.7%.

Embodiment 2

[0031] First the mixed system of tartaric acid (0.5mol, 75g), acetone (890g) and water (61.4g) was warmed up and refluxed until tartaric acid was completely dissolved, then under reflux, formula (II) metoprolol (1mol, 267g) Add the mixed solution of acetone (311.5g) dropwise to the solution, after the dropwise addition, keep it warm at 50-65°C for 1 hour, cool to 0-5°C, stir and crystallize for 1 hour, after the crystallization , suction filtration, drying to obtain formula (I) metoprolol salt 307.57g, productive rate 89.8%.

Embodiment 3

[0033] First the mixed system of tartaric acid (0.5mol, 75g), acetone (890g) and water (61.4g) was warmed up and refluxed until tartaric acid was completely dissolved, then under reflux, formula (II) metoprolol (1mol, 267g) Add the mixed solution of acetone (311.5g) dropwise to the solution, after the dropwise addition, keep it warm at 50-65°C for 0.5 hours, cool to 0-5°C, stir and crystallize for 2 hours, after the crystallization , suction filtration, drying to obtain formula (I) metoprolol salt 320.24g, productive rate 93.5%.

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PUM

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Abstract

The invention relates to a method for preparing a metoprolol salt which is simple to operate, high in yield, good in quality, low in cost and good in environmental-friendliness. According to the method provided by the invention, an acetone / water mixed solvent system is adopted, and an adverse dropping mode, that is, a mode that metoprolol is dropped into an organic acid solution, is adopted, so that the organic acid can be sufficiently dissolved, and a reaction can be sufficiently implemented, the reaction time can be greatly shortened, and the reaction conversion rate and the yield can be increased. The operation procedures are simplified, the time is shortened, the cost is lowered, and moreover, the quality of a product is greatly improved.

Description

technical field [0001] The invention relates to a preparation method of metoprolol salt. Background technique [0002] Metoprolol salt, a commonly used β-receptor blocker, can be used to treat hypertension, angina pectoris, arrhythmia and myocardial infarction, hypertrophic cardiomyopathy, aortic dissection, arrhythmia, hyperthyroidism, cardiac Diseases such as neurosis. Because it can improve the selectivity of the drug action, stabilize the blood drug concentration in the body, increase the valley-peak ratio of the blood drug concentration, reduce blood pressure fluctuations, reduce target organ damage, and reduce the number of administrations, it is convenient for patients to take, and has been favored by cardiovascular patients. generally welcome. [0003] The preparation of metoprolol salt has been reported in many patent documents, usually formula (II) prepares formula (I) through salt-forming reaction, as: Janakraj Karamchand Mehra etc. (Janakraj Karamchand Mehra, A...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C213/08C07C217/32
CPCC07C213/08C07C217/32
Inventor 周国斌何人宝金逸中杨建平
Owner ZHEJIANG YONGTAI PHARMA
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