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Method for preparing high-purity esomeprazole magnesium trihydrate

A high-purity esomeprazole magnesium trihydrate technology is applied in the field of drug synthesis to achieve high yield, good selectivity and high reaction efficiency.

Inactive Publication Date: 2016-03-23
QINGDAO CHENDA BIOLOGICAL SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The object of the present invention is to overcome the defect of existing method for preparing esomeprazole, provide a kind of method that yield is high, selectivity is good and reaction efficiency height is suitable for the preparation of esomeprazole magnesium trihydrate of industrial scale production

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] A method for preparing esomeprazole magnesium trihydrate, comprising the following steps:

[0030] 1) Mix 630g (2mol) of omeprazole sulfide with (R)-1,1'-binaphthyl-2,2'-diamine and inorganic metal salt in 5L of acetone, the mixing condition is: temperature 48°C , and stirred for 1 hour to obtain a mixture M; wherein, the molar ratio of the omeprazole sulfide to (R)-1,1'-binaphthyl-2,2'-diamine and inorganic metal salt is 1: 0.65:0.1, the inorganic metal salt is CoCl 2 .

[0031] 2) At a temperature of 45°C, 30% H 2 o 2 Drop into step 1) in the mixture M and carry out oxidation reaction, add potassium hydroxide methanol solution after reaction finishes, obtain esomeprazole potassium; 2 o 2 Gauge, 30%H 2 o 2 The molar ratio to omeprazole thioether is 1.6; the amount of potassium hydroxide methanol solution added, calculated as potassium hydroxide, is 1.5 to the molar ratio of omeprazole thioether.

[0032] 3) Mix the esomeprazole potassium obtained in step 2) wit...

Embodiment 2

[0034] A method for preparing esomeprazole magnesium trihydrate, comprising the following steps:

[0035] 1) Mix 630g (2mol) of omeprazole sulfide with (R)-1,1'-binaphthalene-2,2'-diamine and inorganic metal salt in 5L of acetone, the mixing condition is: temperature 50°C , and stirred for 1.5 hours to obtain a mixture M; wherein, the molar ratio of the omeprazole sulfide to (R)-1,1'-binaphthyl-2,2'-diamine and inorganic metal salt is 1: 0.8:0.15, the inorganic metal salt is CoSO 4 .

[0036] 2) At a temperature of 38°C, 30% H 2 o 2 Drop into step 1) in the mixture M and carry out oxidation reaction, add potassium hydroxide methanol solution after reaction finishes, obtain esomeprazole potassium; 2 o 2 Gauge, 30%H 2 o 2 The molar ratio to omeprazole thioether is 1.7; the amount of potassium hydroxide methanol solution added, calculated as potassium hydroxide, is 1.3 to the molar ratio of omeprazole thioether.

[0037] 3) Mix the esomeprazole potassium obtained in step ...

Embodiment 3

[0039] A method for preparing esomeprazole magnesium trihydrate, comprising the following steps:

[0040] 1) Mix 630g (2mol) of omeprazole sulfide with (R)-1,1'-binaphthyl-2,2'-diamine and inorganic metal salt in 5L of acetone, the mixing condition is: temperature 45°C , and stirred for 1.5 hours to obtain a mixture M; wherein, the molar ratio of the omeprazole sulfide to (R)-1,1'-binaphthyl-2,2'-diamine and inorganic metal salt is 1: 0.4:0.2, the inorganic metal salt is FeCl 2 .

[0041] 2) At a temperature of 40°C, 30% H 2 o 2 Drop into step 1) in the mixture M and carry out oxidation reaction, add potassium hydroxide methanol solution after reaction finishes, obtain esomeprazole potassium; 2 o 2 Gauge, 30%H 2 o 2 The molar ratio to omeprazole thioether is 1.4; the amount of potassium hydroxide methanol solution added, calculated as potassium hydroxide, is 1.4 to the molar ratio of omeprazole thioether.

[0042] 3) Mix the esomeprazole potassium obtained in step 2) w...

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Abstract

The invention discloses a method for preparing a high-purity esomeprazole magnesium trihydrate. The method comprises the following steps: (1), mixing omeprazole sulfide, (R)-1,1 minute-binaphthyl-2,2 minute-diamine and inorganic metal salt in acetone, thereby obtaining a mixture M; (2), at a condition of 15-45 DEG C, dipping 30% H2O2 into the mixture M of the step (1) to perform an oxidization reaction, and after the oxidization reaction is completed, adding potassium hydroxide and methanol solution, thereby obtaining esomeprazole potassium; (3), mixing the esomeprazole potassium obtained in step (2) with anhydrous magnesium chloride in methyl alcohol, stirring to react, and centrifuging and separating, thereby obtaining the esomeprazole magnesium trihydrate, wherein in step (1), the inorganic metal salt is cobalt (II), iron (II) or magnesium (II) metal salt. The method for preparing the high-purity esomeprazole magnesium trihydrate has high yield, good selectivity and high reaction efficiency, and is suitable for industrial mass production.

Description

technical field [0001] The invention belongs to the field of drug synthesis, in particular to a method for preparing esomeprazole magnesium trihydrate. Background technique [0002] Esomeprazole magnesium (esomeprazolemagnesium), is the S-isomer magnesium salt preparation of omeprazole listed by AstraZeneca, Sweden in 1988, S-(-)-5-methoxy-2-[(4- Methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]benzimidazol-1-ylmagnesium, present in the formulation as esomeprazole magnesium trihydrate. As a new type of proton pump inhibitor, esomeprazole magnesium can inhibit the activity of H / K-ATPase, and is used to treat digestive system diseases such as gastric ulcer, duodenal ulcer and reflux esophagitis caused by excessive gastric acid secretion . [0003] At present, esomeprazole salt is mainly obtained by esomeprazole salification, therefore, the preparation method of esomeprazole not only affects the yield and the purity of esomeprazole, but also affects the yield and purity of eso...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
CPCC07D401/12C07B2200/07
Inventor 陈令浩
Owner QINGDAO CHENDA BIOLOGICAL SCI & TECH
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