New S-omeprazole salts

A technology for omeprazole potassium salt and omeprazole is applied in the field of novel S-omeprazole salt, can solve problems such as poor crystallinity, and achieve the effects of easy processing and storage, and easy large-scale preparation

Inactive Publication Date: 2011-11-16
CHENGDU ORGANIC CHEM CO LTD CHINESE ACAD OF SCI
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  • Application Information

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Problems solved by technology

In 2004, U.S. Patent US20040242642 described a magnesium salt solid obtained by distilling off the methanol in the methanol solution of esomeprazole magnesium salt, then adding water and stirring, and then mixing acetone and water at 0-5°C Method for preparing esomeprazole trihydrate with specific crystal form by stirring and recrystallizing esomeprazole magnesium salt in solvent, but we have confirmed esomeprazole magnesium salt with specifi

Method used

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Examples

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Embodiment Construction

[0042] Example 1: Preparation of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl]-1H-benzimidazole

[0043] 0.348 g (1.5 mmol) of D-di-n-propionamide tartrate was added to the reactor, 7.5 ml of toluene was added, the temperature was raised to 60°C under stirring, and 0.225 ml (0.75 mmol) of Ti(Oi-Pr) was added 4 After 60 minutes, 0.0068 ml (0.375 mmol) of water was added and stirred for another 60 minutes. Cool down to 30°C, add 0.822 g (2.5 mmol) omeprazole precursor thioether, after stirring for 10 minutes, add 0.5 ml (2.7 mmol) 80% CHP dropwise, keep the reaction for 5 hours, the product is not separated, take A small amount of reaction solution is measured by HPLC and enantioselectivity is 80%, by 1 The yield calculated by H NMR internal standard method was 50%.

[0044] Example 2: Preparation of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl]-1H-benzimidazole

[0045] 0.348 g (1.5 mmol) of D-di-n-propionamide tartrate was added to the ...

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Abstract

The invention provides new S-omeprazole salts in special crystal forms, namely an S-omeprazole potassium salt di-ethanol adduct and an S-omeprazole magnesium salt trihydrate. The invention also relates to a method for preparing the S-omeprazole magnesium salt trihydrate with a special crystal form from the S-omeprazole potassium salt di-ethanol adduct. The invention aims to provide a simple method for preparing the S-omeprazole magnesium salt hydrate in the special form by utilizing water, a magnesium source and a cheap organic solvent on the basis of a simple and cheap enantioselectivity oxidation method for preparing new optically pure omeprazole potassium salts.

Description

technical field [0001] The present invention relates to novel S-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl]-1H-benzimidazole The potassium salt diethanolate and the magnesium salt hydrate. More specifically, the present invention relates to S-omeprazole potassium salt diethanolate and magnesium salt hydrate with specific crystal forms. In addition, the present invention also relates to a method for preparing S-omeprazole magnesium salt hydrate with specific crystal form by using S-omeprazole potassium salt diethanolate. Background technique [0002] Compound 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl]-1H-benzimidazole (commonly known as Ogilvy meprazole) and pharmaceutically acceptable salts thereof are described in EP5129. Specific alkali metal salts of omeprazole are described in EP124495. Omeprazole inhibits H + , K + - The activity of ATPase (also known as proton pump), which inhibits gastric acid secretion, has been widely...

Claims

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Application Information

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IPC IPC(8): C07D401/12A61K31/4439A61P1/04
Inventor 邓金根田添朱槿廖建黄晴菲
Owner CHENGDU ORGANIC CHEM CO LTD CHINESE ACAD OF SCI
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