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Sodium rabeprazole preparation method

A technology of rabeprazole sodium and rabeprazole sulfide, applied in the field of preparation of rabeprazole sodium, can solve the problems of incomplete crystallization, low yield, complex reaction process, etc., and achieve short steps and high yield High, easy-to-operate effect

Active Publication Date: 2013-03-06
JIANGSU AOSAIKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method has the following disadvantages: (a) the reaction process is complicated, the equipment investment is large, and the production cycle is long; (b) repeated concentration is required, which easily causes the product to peroxidize and decompose, and the concentrate is syrupy, which is easy to attach to the container wall and stir On the paddle, when other solvents are used for crystallization, incomplete crystallization and low yield may occur; (c) Wastewater contains a large amount of inorganic salts and organic solvents, which is easy to pollute the environment
There are also certain problems in this method: (a) the use of pyridine with reproductive toxicity and carcinogenic methylene chloride is harmful to the human body and the environment; The decomposition of rabeprazole sodium and the increase of peroxidation impurities reduce the quality of the product and are not conducive to industrial production; (c) unreacted sulfides are insoluble in alkaline water, and unreacted raw materials will be extracted together during extraction with dichloromethane , will be precipitated together with the product in the follow-up, resulting in a great reduction in the quality of the product

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Add 10g of rabeprazole sulfide into 50ml of water, add 3g of sodium hydroxide dissolved in 30ml of water under stirring, cool the reaction solution to 0°C, add 60g of sodium hypochlorite solution containing 4% active chlorine dropwise, keep the reaction for 12h, add dropwise Dissolve 15 g of sodium thiosulfate in 30 ml of water to quench the reaction, stir for 0.5 h and filter, pour the filtrate into 200 g of saturated saline under stirring, stir at room temperature for 1 h, filter, and dry the filter cake under reduced pressure to obtain rabeprazole sodium solid 9.14 g, yield 82.3%. HPLC purity 99.82%.

Embodiment 2

[0032] Add 10g of rabeprazole sulfide into 30ml of water, cool the reaction solution to 5°C, slowly add 7.2g of sodium tert-butoxide under stirring, then dropwise add 40g of sodium hypochlorite solution containing 4% active chlorine, keep the reaction for 12h, add dropwise Dissolve 5g of sodium thiosulfate in 30ml of water to quench the reaction, stir for 0.5h and filter, pour the filtrate into 100g of saturated saline under stirring, stir at room temperature for 1h, filter, and dry the filter cake under reduced pressure to obtain rabeprazole sodium solid 8.6 g, yield 77.4%. HPLC purity 99.87%.

Embodiment 3

[0034] Add 10g of rabeprazole sulfide into 50ml of water, cool the reaction solution to 10°C, slowly add 3.3g of sodium methoxide under stirring, then dropwise add 60g of sodium hypochlorite solution containing 4% active chlorine, keep the reaction for 12h, add dropwise to dissolve in 30ml 15 g of sodium thiosulfate in water quenched the reaction, stirred for 0.5 h and then filtered, poured the filtrate into 300 g of saturated saline under stirring, stirred at room temperature for 1 h, filtered, and dried the filter cake under reduced pressure to obtain 8.8 g of rabeprazole sodium solids, collected The rate is 79.2%. HPLC purity 99.75%.

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PUM

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Abstract

The present invention relates to a sodium rabeprazole preparation method, which comprises the following steps: adding rabeprazole thioether to water, adding an alkaline material containing sodium ions, adding a sodium hypochlorite solution in a dropwise manner at a temperature of 0-20 DEG C, carrying out a stirring reaction for 12-18 h, filtering the reaction solution, adding a saturated salt solution to the filtrate, stirring, filtering, and carrying out reduced pressure drying on the obtained solid to obtain the sodium rabeprazole. According to the present invention, extraction and concentration are not required, process steps and organic solvent use are reduced, safety and environmental protection are provided, cost is low, and the method is suitable for industrial production.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a preparation method of rabeprazole sodium. Background technique [0002] Rabeprazole, its chemical name is: 2-[[4-(3-methoxypropoxy)-3-methylpyridine]-2-methyl]sulfinyl]-1H-benzimidazole. Rabeprazole sodium is a new generation of proton pump inhibitors following omeprazole and lansoprazole. It has a high pKa value and is rapidly activated in vivo. It inhibits the activity of H+ / K+-ATPase in gastric parietal cells. , thereby inhibiting the secretion of gastric acid. Clinically, it is mainly used to treat peptic ulcer, gastroesophageal reflux disease, Zoller-Ellison syndrome and other diseases. It was first launched in Japan in 1997, and then in Europe, the United States, and China respectively. The dosage form is enteric-coated tablets. Studies have shown that rabeprazole sodium has a stronger inhibitory effect on H+ / K+-ATPase activity than omeprazole, and the inhibition can...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
Inventor 赵俊宗在伟文伟河
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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