A kind of preparation method of esomeprazole magnesium

A technology of esomeprazole magnesium and azole thioether, which is applied in the field of pharmaceutical preparation and can solve problems such as inconvenient operation, being caught in it, and difficult to remove impurities
CN110305108BActive Publication Date: 2022-05-03湖南协创药品开发有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
湖南协创药品开发有限公司
Publication Date
2022-05-03

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Abstract

The invention relates to a preparation method of esomeprazole magnesium, comprising the following steps: mixing omeprazole sulfide, diethyl tartrate and isopropyl titanate, adding diisopropylethylamine, stirring, Add cumene hydroperoxide dropwise, separate to obtain an oily substance; add strong base, stir, then add strong base one by one, extract, wash, do TLC monitoring, stop adding strong base when there is basically no spot; cool down, crystallize, Filter and rinse to obtain esomeprazole salt; dissolve esomeprazole salt in water, cool down to below 20°C, adjust pH, add magnesium sulfate heptahydrate aqueous solution dropwise, after the dropwise addition, stir and filter , rinse, and dry to obtain crude esomeprazole magnesium; dissolve the crude esomeprazole magnesium with methanol, decolorize activated carbon, filter, concentrate, dissolve again, add acetone aqueous solution, stir, suction filter, dry, The esomeprazole magnesium is obtained, and the product prepared by the invention has high purity, good yield and less impurities.
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Description

technical field

[0001] The invention belongs to the field of medicine preparation methods, in particular to a preparation method of esomeprazole magnesium. Background technique

[0002] Esomeprazole is a proton pump inhibitor that reduces gastric acid secretion and prevents the formation of gastric acid by inhibiting the H+ / K+-ATPase of gastric parietal cells. It is used for gastroesophageal reflux disease (GORD) including erosive reflux The initial and long-term treatment of liquid esophagitis (including erosive esophagitis), developed by AstraZeneca Pharmaceuticals Co., Ltd., is listed in the United States under the trade name "Nexium".

[0003] Esomeprazole magnesium is the magnesium salt of esomeprazole, and Astra Corporation indicated in CN1110477 that sodium salt and magnesium salt are the best esomeprazole salts of efficacy. Lin Qing's "Preparation, Characterization and Mutual Transformation of Esomeprazole Magnesium Polymorphs" shows that esomeprazole magnesium trih...

Claims

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