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Preparation technology of lansoprazole

A technology for the preparation of lansoprazole and a preparation process, which is applied in the field of preparation of pharmaceutical compounds, can solve the problems of backward raw material preparation process, uneasy control of the crystallization process, unstable product performance, etc. It is simple and easy to meet equipment requirements, shorten the production cycle, The effect of material stabilization

Active Publication Date: 2017-07-07
HENAN KANGDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Compared with similar foreign products, domestic lansoprazole has gaps in low yield, too small crystal size, uneven particle size distribution, and low purity.
In addition, as far as the current technological situation is concerned, in the preparation process of lansoprazole, the process is complex, the production cycle is long, and the crystallization process is difficult to control.
The existence of these problems leads to poor and unstable product quality on the one hand, and also leads to an increase in production costs and waste of raw materials to a certain extent.
With the expansion of the market, large-scale production of products has disadvantages such as backward raw materials and preparation technology, high cost, and unstable product performance.

Method used

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  • Preparation technology of lansoprazole
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  • Preparation technology of lansoprazole

Examples

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Effect test

Embodiment 1

[0031] A preparation technique for Lansoprazole, comprising the following steps:

[0032] (a) In a clean glass kettle, first add 6L of anhydrous methanol, then add 0.7kg of 2-mercaptobenzimidazole (raw material A) and 0.5kg of solid sodium hydroxide under stirring, raise the temperature to 40-50°C, and control the temperature. After stirring and dissolving, add 1kg of 2-chloromethyl-3-methyl-4-(2,2,2,-trifluoroethoxy)pyridine hydrochloride (raw material B) to dissolve, react for 2 hours, add appropriate amount of purification water, cool down to room temperature, spin filter, wash the precipitate with purified water, spin dry, and vacuum dry at 45°C to obtain intermediate C;

[0033] (b) Add intermediate C to 10L of 95% ethanol, control the temperature at 10-15°C, stir and dissolve, then add a mixture of 0.6kg of 30% hydrogen peroxide, 0.02kg of catalyst and 0.3 kg of ethanol, and react for 2 hours under temperature control. After HPLC detection, the residue of intermediate C...

Embodiment 2

[0036] A preparation technique for Lansoprazole, comprising the following steps:

[0037] (a) In a clean glass kettle, first add 7L of anhydrous methanol, then add 0.8kg of 2-mercaptobenzimidazole (raw material A) and 0.6kg of solid sodium hydroxide under stirring, raise the temperature to 40-50°C, and control the temperature. After stirring and dissolving, add 1kg of 2-chloromethyl-3-methyl-4-(2,2,2,-trifluoroethoxy)pyridine hydrochloride (raw material B) to dissolve, react for 2 hours, add appropriate amount of purification water, cool down to room temperature, spin filter, wash the precipitate with purified water, spin dry, and vacuum dry at 45°C to obtain Intermediate C.

[0038] (b) In a clean glass kettle, first add 10L of 95% ethanol, then add the intermediate C obtained above under stirring, control the temperature at 10-15°C, stir and dissolve, then add 0.6kg of 30% hydrogen peroxide and 0.05kg of catalyst The mixed solution mixed with 0.48 kg ethanol was reacted at ...

Embodiment 3

[0041] A preparation technique for Lansoprazole, comprising the following steps:

[0042] (a) In a clean glass kettle, first add 8L of anhydrous methanol, then add 0.8kg of 2-mercaptobenzimidazole (raw material A) and 0.6kg of solid sodium hydroxide under stirring, raise the temperature to 40-50°C, control the temperature, and stir After dissolving, add 1 kg of 2-chloromethyl-3-methyl-4-(2,2,2,-trifluoroethoxy)pyridine hydrochloride (raw material B) to dissolve, react for 2 hours, add appropriate amount of purified water, Cool down to room temperature, spin filter, wash with purified water, spin dry, and vacuum dry at 45°C to obtain intermediate C.

[0043] (b) In a clean glass kettle, first add 10L of 95% ethanol, then add the intermediate C obtained above under stirring, control the temperature at 10-15°C, stir and dissolve, then add 0.3kg of 30% hydrogen peroxide and 0.05kg of catalyst The mixed solution mixed with 0.24 kg ethanol was reacted for 2 hours under temperature ...

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Abstract

The invention provides a preparation technology of lansoprazole. The preparation technology comprises the following steps that 1, a raw material A 2-mercapto benzimidazole is dissolved into methanol in the presence of alkali, a raw material B 2-chloromethyl-3-methyl-4-(2,2,2,-trifluoroethoxyl)pyridine hydrochloride is added for a reaction, filtering is conducted by adding water, obtained precipitates are washed and dried, and then an intermediate C [[[3-methyl-4-(2,2,2,-trifluoroethoxyl)-2-pyridyl]methyl]sulfydryl]-H-benzimidazole is obtained; the intermediate C is dissolved into ethanol, a mixed solution of hydrogen peroxide, a catalyst and ethanol is added for a reaction, filtering is conducted by adding water, obtained precipitates are washed, and then the lansoprazole is obtained. According to the preparation technology, the yield is increased, the cost is reduced, the production cycle is shortened, and the preparation technology is more suitable for industrialized production.

Description

technical field [0001] The invention belongs to the technical field of preparation of pharmaceutical compounds, in particular to a preparation process of lansoprazole. Background technique [0002] Lansoprazole (Lansoprazole), its chemical name is: 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl ]-1H-benzimidazole, which is a benzimidazole compound, is transferred to the gastric mucosa after oral absorption, and is converted into an active metabolite under acidic conditions, which specifically inhibits gastric parietal cell H + / K + The ATPase system thus blocks gastric acid secretion. Lansoprazole inhibits basal gastric acid secretion and gastric acid secretion under stimulation in a dose-dependent manner, has no antagonistic effect on choline and histamine H2 receptors, and is used for the treatment of gastric ulcer, duodenal ulcer, and reflux esophagitis , Zoe-Ellison syndrome (gastrinoma). [0003] Digestive system disease is one of the common frequ...

Claims

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Application Information

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IPC IPC(8): C07D401/12
Inventor 孙津鸽李志军李文杰高德瀛刘红坤韩新正李红德
Owner HENAN KANGDA PHARMA
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