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Preparation method of pantoprazole sodium

A technology of pantoprazole sodium and benzimidazole, which is applied in the field of preparation of pantoprazole sodium, can solve the problems of many side reactions and cumbersome steps, and achieve the effects of easy control, strong safety, simple and efficient operation

Inactive Publication Date: 2013-01-23
JIANGSU HAICI BIOLOGICAL PHARMA CO LTD OF YANGTZE RIVER PHARMA GRP
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

[0006] Chinese patent CN101475561A discloses the preparation method of pantoprazole sodium monohydrate, and this method step is loaded down with trivial details, and side reaction is more

Method used

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  • Preparation method of pantoprazole sodium
  • Preparation method of pantoprazole sodium

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Embodiment 1

[0033] Embodiment 1 prepares pantoprazole sodium

[0034] Prepare pantoprazole sodium, comprises the following steps:

[0035] 1) Preparation of compound 2-chloromethyl-3,4-dimethoxypyridine hydrochloride (Ⅲ)

[0036] Add 9.22kg of toluene, add 1.5kg of 2-hydroxymethyl-3,4-dimethoxypyridine at room temperature, cool down to 3°C~10°C, add 1.63kg of chloride within 1~2 hours at 3-10°C After the addition of sulfoxide, keep stirring at 5-10°C for 1 hour, heat up to 35°C-40°C within 1 hour, and keep warm at 35-40°C for 4 hours. After the reaction was detected by TLC, the temperature was controlled at 35-40°C, vacuum distilled thionyl chloride for 3-4 hours, 9kg of toluene was added, the temperature was lowered to 20-25°C, centrifugal suction filtration, 0.64L toluene washed the filter cake, and dried to obtain intermediate Body I (2-chloromethyl-3,4-dimethoxypyridine hydrochloride), air-dried at 50-55°C for 6-8 hours.

[0037] ) Preparation of compound 5-difluoromethoxy-2-[...

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Abstract

The invention provides a preparation method of pantoprazole sodium. The method comprises the following steps of: 1) generating 2-chloromethyl-3,4-dimethoxypyridine hydrochloride (III) by taking 2-hydroxymethyl-3,4-dimethoxypyridine (II) as the start raw material in the presence of chloride; 2) condensing the obtained compound (III) with 5-difluoromethoxy-2-sulfydryl-1H-benzimidazole in alkaline conditions in the presence of inorganic base to generate 5-difluoromethoxy-2-[(3,4-dimethoxy-2-pyridyl)methyl]thioxo-1H-benzimidazole (IV); and 3) salifying the obtained compound (IV) with sodium hydroxide, and oxidizing with an oxidizing agent to generate 5-difluoromethoxy-2-[(3,4-dimethoxy-2-pyridyl)methyl]sulfinyl-1H-benzimidazole sodium, namely pantoprazole sodium (I). According to the invention, the operation is simple and efficient, the reaction conditions are mild, the safety is high, the control is easy, the yield is relatively high, and the method is suitable for industrial production.

Description

technical field [0001] The invention relates to a preparation method of pantoprazole sodium, which belongs to the technical field of pharmaceutical production. Background technique [0002] Pantoprazole Sodium (Pantoprazole Sodium), its chemical name is: 5-difluoromethoxy-2-[(3,4-dimethoxy-2-pyridyl)-methyl]-sulfinyl- 1H benzimidazole sodium salt monohydrate, its structural formula is: [0003] [0004] Pantoprazole sodium is the third-generation proton pump inhibitor after omeprazole and lansoprazole. Pantoprazole sodium is a proton pump inhibitor for gastric parietal cells, which is relatively stable under neutral and weak acidic conditions. It is rapidly activated under strong acidic conditions, and its pH-dependent activation properties make it highly resistant to H + 、K + - The action of ATPase has better selectivity. This product can specifically inhibit the release of H on the secretory microtubules formed by the apical membrane of the parietal cells and the tu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
Inventor 王伟王庆辉冯建鹏陈元龙朱圣红祝传宝陆良喆
Owner JIANGSU HAICI BIOLOGICAL PHARMA CO LTD OF YANGTZE RIVER PHARMA GRP
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