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Preparation method of rabeprazole sodium crystal type compound

The technology of rabeprazole sodium and compound is applied in the field of preparation of rabeprazole sodium crystal compound, can solve the problems of high price, limited consumer groups, etc., and achieves the effects of low cost, low manufacturing cost and stable property of goods

Active Publication Date: 2013-08-07
SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, rabeprazole is mainly sourced from Japan, its price is high, and its consumer groups are limited

Method used

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  • Preparation method of rabeprazole sodium crystal type compound
  • Preparation method of rabeprazole sodium crystal type compound
  • Preparation method of rabeprazole sodium crystal type compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] This example provides a preparation method of rabeprazole sodium crystal form compound, which is 2-mercaptobenzimidazole, 2-chloromethyl-3-methyl-4-methoxypropoxypyridine hydrochloride As a raw material, the final product is obtained through condensation, oxidation and salt-forming reactions, which includes the following preparation steps:

[0028] Condensation reaction: Prepare 32.6kg of methanol in the first clean reaction tank, stir at a speed of 35Hz, drop in 25.00kg of 2-chloromethyl-3-methyl-4-methoxypropoxypyridine hydrochloride, stir Dissolve and prepare a methanol solution of 2-chloromethyl-3-methyl-4-methoxypropoxypyridine hydrochloride for later use.

[0029] Prepare 98.8kg of methanol in the second clean reaction tank, add 8.15kg of sodium hydroxide under stirring at a speed of 40Hz, stir evenly and control the temperature at 20-25°C, put in 14.11kg of 2-mercaptobenzimidazole, and heat up to 50-60°C , add the methanol solution of 2-chloromethyl-3-methyl-4-m...

Embodiment 2

[0040] This example provides a preparation method of rabeprazole sodium crystal form compound, which is 2-mercaptobenzimidazole, 2-chloromethyl-3-methyl-4-methoxypropoxypyridine hydrochloride As a raw material, the final product is obtained through condensation, oxidation and salt-forming reactions, which includes the following preparation steps:

[0041] Condensation reaction: Prepare 32.6kg of methanol in the first clean reaction tank, stir at a speed of 35Hz, drop in 22.8kg of 2-chloromethyl-3-methyl-4-methoxypropoxypyridine hydrochloride, stir Dissolve and prepare a methanol solution of 2-chloromethyl-3-methyl-4-methoxypropoxypyridine hydrochloride for later use.

[0042] Prepare 81.5kg of methanol in the second clean reaction tank, add 6.52kg of sodium hydroxide under stirring at a speed of 40Hz, stir evenly and control the temperature at 20-25°C, put in 8.15kg of 2-mercaptobenzimidazole, and heat up to 50-60°C , add the methanol solution of 2-chloromethyl-3-methyl-4-met...

Embodiment 3

[0046] This example provides a preparation method of rabeprazole sodium crystal form compound, which is 2-mercaptobenzimidazole, 2-chloromethyl-3-methyl-4-methoxypropoxypyridine hydrochloride As a raw material, the final product is obtained through condensation, oxidation and salt-forming reactions, which includes the following preparation steps:

[0047] Condensation reaction: Prepare 32.6kg and 29.3kg of A in the first clean reaction tank, stir and dissolve, and prepare a methanol solution of 2-chloromethyl-3-methyl-4-methoxypropoxypyridine hydrochloride, spare.

[0048] Prepare 98.8kg of methanol in the second clean reaction tank, add 9.88kg of sodium hydroxide under stirring at a speed of 40Hz, stir evenly and control the temperature at 20-25°C, put in 19.76kg of 2-mercaptobenzimidazole, and heat up to 50-60°C , add the methanol solution of 2-chloromethyl-3-methyl-4-methoxypropoxypyridine hydrochloride prepared above at a temperature of 50-60°C, and add in about 30 minute...

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Abstract

The invention relates to the field of medicine production and in particular relates to a preparation method of a rabeprazole sodium crystal type compound. The preparation method of the rabeprazole sodium crystal type compound comprises the following steps of: by taking 2-mercapto benzimidazole and 2-chloromethyl-3-methyl-4-methoxy propoxy pyridine hydrochloride as raw materials and carrying out a condensation reaction to prepare rabeprazole thioether, and subsequently carrying out an oxidation reaction via the rabeprazole thioether and carrying out salt forming reaction via rabeprazole and sodium hydroxide to acquire the rabeprazole sodium. According to the preparation method of the rabeprazole sodium crystal type compound, the raw materials are low in cost and easy to purchase; samples are basically invariant in related substances and contents under the condition with high temperature and high humidity; the articles are stable in property and low in overall manufacturing cost; and the preparation method of the rabeprazole sodium crystal type compound has the advantages of strictly controlling the temperatures in the steps, being less in by-products, high in yield and non-toxic, and also has the advantages of being short in production period and further improving the production efficiency.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a preparation method of rabeprazole sodium crystal form compound. Background technique [0002] Peptic ulcer is a common and frequently-occurring disease, which brings great suffering to patients and reduces the quality of life. Drug treatment of peptic ulcer has become one of the focuses and hotspots of current research and development. Proton pump inhibitors (Proton pump inhibitors, PPIS), which came out in the 1980s, are currently the most effective drugs for treating peptic ulcer disease and inhibiting gastric acid secretion. - ATPase activity, thereby inhibiting gastric acid secretion. [0003] The first proton pump inhibitor was omeprazole, which was successfully developed by Astra in 1988 and was first marketed in Sweden. Following omeprazole, the pharmaceutical industry has successively developed proton pump inhibitors such as lansoprazole, pantoprazole, esomeprazole and rabep...

Claims

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Application Information

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IPC IPC(8): C07D401/12
Inventor 李晓峰刘明霞曹传张兆永罗兆亮
Owner SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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