Rabeprazole preparation method

A technology of rabeprazole and dichloromethane, which is applied in the field of pharmaceutical preparation, can solve the problems of high manufacturing cost and complicated manufacturing process, and achieve the effects of good product quality and simple preparation method.

Inactive Publication Date: 2015-07-01
李磊
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Because currently in the process of producing rabeprazole, the m...

Method used

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Embodiment Construction

[0006] Now in conjunction with the present invention for further detailed description.

[0007] A kind of preparation method of rabeprazole of the present invention, concrete steps are as follows: 2,3-dimethyl-4-nitropyridine-N-oxide is dissolved in dichloromethane, trifluoroacetic anhydride is added dropwise, adds Complete reflux for 4 hours, evaporate excess trifluoroacetic anhydride, add dichloromethane, cool to room temperature, add triethylamine and 2-mercaptobenzimidazole, react until complete, evaporate solvent, add ethanol and water, stir for 30 minutes, Filtration to get 2-[[(3-methyl-4-nitro-2-pyridyl)methyl]sulfur]-1H-benzimidazole, the compound and potassium carbonate suspended in 3-methoxy 1-propane In alcohol and isopropanol, heat at 85°C for 48h, cool to 20°C, add chloroform, filter, wash the filtrate with water, concentrate the organic layer to dryness under reduced pressure, and obtain 2-[[[3-methyl- 4-(3-Methoxypropoxy)-2-pyridyl]methyl]sulfur]-1H-benzimidaz...

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Abstract

The invention relates to a rabeprazole preparation method. The method concretely comprises the following steps: dissolving 2,3-dimethyl-4-nitropyridin-N-oxide in dichloromethane, adding trifluoroacetic anhydride in a dropwise manner, distilling off excess trifluoroacetic anhydride, adding dichloromethane, adding triethylamine and 2-mercaptobenzimidazole, adding ethanol and water, stirring for 30min, filtering to obtain 2-[[(3-methyl-4-nitro-2-pyridyl)methyl]thio]-1H-benzimidazole, carrying out column chromatography on the obtained residue to obtain 2-[[(3-methyl-4-(3-methoxypropanolato)-2-pyridyl)methyl]thio]-1H-benzimidazole, adding a dichloromethane solution of m-CPBA, adjusting the pH value to 13.0 by using 10% sodium hydroxide, separating out the obtained water layer, and adding dichloromethane to obtain the product rabeprazole. The rabeprazole preparation method is simple, and the quality of the product is good.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to a preparation method of rabeprazole. Background technique [0002] Rabeprazole sodium is a drug that inhibits secretion and is a substitute for benzimidazole. It has no anticholinergic and anti-H2 histamine properties, but it can attach to the surface of gastric parietal cells and inhibit gastric acid production by inhibiting H+ / K+-ATPase secretion. This enzyme system is regarded as an acid proton pump, so rabeprazole sodium acts as a proton pump inhibitor in the stomach to block the production of gastric acid, and this effect is dose-related. Animal experiments have confirmed that rabeprazole sodium can be excreted from plasma and gastric mucosa shortly after administration. Because currently it is in the process of producing rabeprazole, the manufacturing process is complicated and the manufacturing cost is high. Contents of the invention [0003] The technical problem ...

Claims

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Application Information

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IPC IPC(8): C07D401/12
CPCC07D401/12
Inventor 李磊
Owner 李磊
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