Synthetic technology of omeprazole

A technology of omeprazole and synthesis process, applied in the field of omeprazole synthesis technology, can solve the problem of high impurities, and achieve the effects of controlling the conversion of impurities, reducing costs and reducing residues

Inactive Publication Date: 2019-10-25
ZHEJIANG JINHUA CONBA BIO PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The application provides a synthesis process of omeprazole to improve or alleviate the problem of high impurities in existing omeprazole products

Method used

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  • Synthetic technology of omeprazole

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] A kind of Omeprazole synthetic technique, it comprises the following steps:

[0083] (1) Add 37g of chloride into 185ml of methanol, stir and dissolve to obtain a chloride solution.

[0084] (2) Add 14 g of sodium hydroxide into 185 ml of methanol, stir to dissolve, add 30 g of benzimidazole derivatives, and obtain an alkaline solution of benzimidazole derivatives.

[0085] The chloride solution obtained in the step (1) is added dropwise to the alkaline solution of the benzimidazole derivative to cause condensation reaction between the two.

[0086] Wherein, during the dropping process, the temperature is controlled at 10°C to 20°C. After the dropwise addition, the temperature is controlled at 10°C to 20°C, and the stirring reaction is continued for 1 hour. After the condensation reaction is completed, the obtained reaction solution is cooled at 5°C to 10°C. Crystallization, centrifugal filtration, after washing the obtained precipitated crystal with 1L of purified wat...

Embodiment 2

[0092] A kind of Omeprazole synthetic technique, it comprises the following steps:

[0093] (1) Add 37g of chloride into 185ml of methanol, stir and dissolve to obtain chloride solution.

[0094] (2) Add 14g of sodium hydroxide into 185ml of methanol, stir and dissolve, add 31g of benzimidazole derivatives to obtain an alkaline solution of benzimidazole derivatives.

[0095] The chloride solution obtained in the step (1) is added dropwise to the alkaline solution of the benzimidazole derivative to cause condensation reaction between the two.

[0096]Wherein, during the dropping process, the temperature is controlled at 10°C to 20°C. After the dropwise addition is completed, the temperature is controlled at 10°C to 20°C, and the stirring reaction is continued for 1 hour until the condensation reaction is completed, and the obtained reaction solution is cooled and crystallized at 5°C to 10°C. Centrifugal filtration, the obtained precipitated crystals were added to 70ml of metha...

Embodiment 3

[0102] A kind of Omeprazole synthetic technique, it comprises the following steps:

[0103] (1) Add 37g of chloride into 139ml of methanol, stir and dissolve to obtain a chloride solution.

[0104] (2) Add 13g of sodium hydroxide into 116ml of methanol, stir and dissolve, add 31g of benzimidazole derivatives to obtain an alkaline solution of benzimidazole derivatives.

[0105] The chloride solution obtained in the step (1) is added dropwise to the alkaline solution of the benzimidazole derivative to cause condensation reaction between the two.

[0106] Wherein, during the dropping process, the temperature is controlled at 10° C. to 20° C., after the dropwise addition is completed, the temperature is controlled at 10° C. to 20° C., and the stirring reaction is continued for 1 hour to obtain a reaction solution.

[0107] (3) Get 25ml of hydrogen peroxide with a mass concentration of 35% and 4ml of purified water to prepare hydrogen peroxide with a mass concentration of 30% as a...

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Abstract

The invention discloses a synthetic technology of omeprazole, and relates to the field of pharmacy. The synthetic technology comprises the following steps that a chloride solution and an alkaline solution of a benzimidazole derivative are mixed to generate a condensation reaction, in the presence of a catalyst and under the alkaline condition, a product of omeprazole sulfur ether obtained after the condensation reaction has an oxidation reaction under the action of an oxidant to generate the omeprazole, and the molar ratio of chloride and the benzimidazole derivative is 1 to (1.4-1.6). According to the synthetic technology of the omeprazole, in the oxidation reaction process, the alkaline condition is kept for a reaction, the conversion of impurities is effectively controlled, and the impurities contained by the meoprazole are reduced, meanwhile, the proportion of main raw materials is reasonably adjusted, reaction by-products are reduced, the residue of materials which are not reactedcompletely in products is lowered, and the impurities and the cost are lowered.

Description

technical field [0001] The application relates to the field of pharmacy, in particular to a synthesis process of omeprazole. Background technique [0002] The omeprazole product produced by the existing omeprazole synthesis process has relatively high impurities, which cannot be removed in the oxidation and refining process, resulting in relatively high impurities in the final product. Contents of the invention [0003] The application provides a synthesis process of omeprazole to improve or alleviate the problem of high impurities in existing omeprazole products. [0004] A kind of omeprazole synthetic technique provided according to the embodiment of the present application, it comprises the following steps: [0005] The chloride solution is mixed with the alkaline solution of benzimidazole derivatives to undergo condensation reaction. In the presence of a catalyst and under alkaline conditions, the omeprazole sulfide product obtained after the condensation reaction und...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
CPCC07D401/12
Inventor 陈冠华金鑫蒋红梅金轶俊黄卫莲叶思婷
Owner ZHEJIANG JINHUA CONBA BIO PHARM CO LTD
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