Preparation method of esomeprazole magnesium

A kind of technology of esomeprazole magnesium, esomeprazole magnesium crude product, is applied in the preparation field of esomeprazole magnesium, can solve undisclosed esomeprazole magnesium purification and purification method, separation and purification difficulty etc. problems, to achieve the effect of meeting pharmaceutical needs, reducing polarity, and morphological stability

Active Publication Date: 2014-03-12
NANJING YOKO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Disclosed in CN1110477A is a kind of generation esomeprazole magnesium salt with magnesium chloride and esomeprazole sodium reaction, but because magnesium chloride is all soluble in water and used alcoholic solvent, brings bigger difficulty to follow-up separation and purification , and the patent does not disclose the purification and refining method of esomeprazole magnesium

Method used

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  • Preparation method of esomeprazole magnesium
  • Preparation method of esomeprazole magnesium
  • Preparation method of esomeprazole magnesium

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Embodiment 1

[0023] The preparation of embodiment 1 esomeprazole

[0024] According to the method disclosed in CN1157614A, prepare esomeprazole 35.2Kg, HPLC purity is 69.4%, standby.

Embodiment 2

[0025] The preparation of embodiment 2 esomeprazole magnesium

[0026] (1) take Example 1 The prepared esomeprazole 6.5Kg was dissolved into a concentrated solution with 1.7L of methanol, and 1Kg of KOH solid was weighed and dissolved in 6L of purified water;

[0027] (2) Slowly add aqueous potassium hydroxide solution to the methanol solution of esomeprazole being stirred, after adding, stir and react for 1 hour to obtain light yellow transparent esomeprazole potassium salt solution;

[0028] (3) In addition, weigh 1.0Kg of anhydrous magnesium sulfate and dissolve it in 40L of purified water to obtain a clear liquid;

[0029] (4) Slowly add the previously obtained esomeprazole potassium solution dropwise to the mechanically stirred magnesium sulfate aqueous solution, stir and react for 1 hour after the dropwise addition, filter with suction, and dry in vacuum to obtain 6.0Kg esomeprazole Magnesium, HPLC purity 97.8%, water content 6.4%.

Embodiment 3

[0030] The preparation of embodiment 3 esomeprazole magnesium

[0031] (1) take Example 1 The prepared esomeprazole 6.5Kg was dissolved into a concentrated solution with 3.2L of methanol, and 1.2Kg of KOH solid was weighed and dissolved in 5L of purified water;

[0032] (2) Slowly add the methanol solution of esomeprazole into the stirring potassium hydroxide aqueous solution, after the dripping is completed, stir and react for 1 hour to obtain a light yellow transparent potassium salt solution of esomeprazole;

[0033] (3) In addition, 1.5Kg of anhydrous magnesium sulfate was weighed and dissolved in 50L of purified water to obtain a clear liquid;

[0034] (4) Slowly add the previously obtained esomeprazole potassium solution dropwise to the mechanically stirred magnesium sulfate aqueous solution, stir and react for 1 hour after the dropwise addition, filter with suction, and dry in vacuum to obtain 5.9Kg esomeprazole Magnesium, HPLC purity 98.1%, water content 6.1%.

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Abstract

The invention relates to a preparation method of esomeprazole magnesium. The method comprises the steps that: esomeprazole is dissolved in an organic solvent; a potassium-containing alkali or salt is subjected to a reaction with esomeprazole, such that esomeprazole potassium is produced; and esomeprazole potassium is subjected to a displacement reaction with a magnesium salt, such that esomeprazole magnesium is prepared. The invention also relates to a refining method of esomeprazole magnesium. With the method provided by the invention, the purity of the prepared esomeprazole magnesium is higher than 99.9%, the yield is higher than 82%, and esomeprazole magnesium has good morphological stability. With the method, requirements by factory pharmacy for purity and yield can be satisfied.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a preparation method of esomeprazole magnesium. Background technique [0002] P. L. Lindberg et al. disclosed in US5877192 that Omeprazole (Omeprazole) has two isomers, right-handed (R-) and left-handed (S-), among which the efficacy of the S-isomer is obviously superior. In R-omeprazole, and Esomeprazole (Esomeprazole) is the S-configuration isomer of omeprazole. The results of the study show that esomeprazole has higher bioavailability and longer half-life after oral administration than omeprazole racemate, can reduce acidity more effectively, significantly improve the cure rate of erosive esophagitis, and is more rapid Effectively relieves symptoms such as heartburn. [0003] Astra disclosed pharmaceutically acceptable salts of esomeprazole in CN1110477A, ​​including its sodium, magnesium, lithium, potassium, calcium and ammonium salts, and believed that its sodium salt an...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D401/12
Inventor 闵涛徐晓霞刘春猛顾传虎
Owner NANJING YOKO PHARMA
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