Preparation method of lansoprazole crystal type compound

A technology of lansoprazole crystals and compounds, which is applied in the field of drug preparation, can solve the problems of high cost and high price of raw materials for preparation, and achieve the effects of low manufacturing cost, short production cycle and few by-products

Active Publication Date: 2013-08-07
SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Lansoprazole is manufactured by Japan's Takeda Pharmaceutical Co., Ltd., and its preparation raw material cost is high, and the price is expensive

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] This embodiment provides a method for preparing a lansoprazole crystal compound, which uses 2-mercaptobenzimidazole as a raw material, undergoes condensation and oxidation reactions, and is then refined. The specific preparation process is as follows:

[0026] 1) Preparation of intermediates: Add 1000ml ethanol solution to a three-necked flask, mix 71.2g 2-mercaptobenzimidazole with 126.5g 2-chloromethyl-3-methyl-4-(2,2,2-trifluoroethoxy base) pyridine hydrochloride into a three-necked flask. Start stirring and add 53g of sodium carbonate, then add 600ml of ethanol solution, heat to reflux for 1.5 hours, evaporate the solvent under reduced pressure, wash with water, and dry to obtain 151g of a white solid intermediate, with a yield of 93%.

[0027] 2) Preparation of Lansoprazole: Add step (1) gained intermediate 130g in a three-necked flask with 1200ml chloroform, stir to make it dissolve, and cool the three-necked flask with ice-salt water bath, so that the temperature...

Embodiment 2

[0030] This embodiment provides a method for preparing a lansoprazole crystal compound, which uses 2-mercaptobenzimidazole as a raw material, undergoes condensation and oxidation reactions, and is then refined. The specific preparation process is as follows:

[0031] 1) Preparation of intermediates: Add 925ml ethanol solution into a three-necked flask, mix 71.2g 2-mercaptobenzimidazole with 121g 2-chloromethyl-3-methyl-4-(2,2,2-trifluoroethoxy ) pyridine hydrochloride into the three-necked flask. Stirring was started and 49.8 g of sodium carbonate was added, followed by 600 ml of ethanol solution. After heating to reflux for 1.5 hours, the solvent was evaporated under reduced pressure, washed with water, and dried to obtain a white solid intermediate.

[0032] Two) the preparation of lansoprazole: in the there-necked flask of 1170ml chloroform, add step (1) gained intermediate 130g, stir and make it dissolve, and the three-necked flask is cooled with an ice-salt water bath, so...

Embodiment 3

[0035] This embodiment provides a method for preparing a lansoprazole crystal compound, which uses 2-mercaptobenzimidazole as a raw material, undergoes condensation and oxidation reactions, and is then refined. The specific preparation process is as follows:

[0036] 1) Preparation of intermediates: Add 1068ml ethanol solution to a three-necked flask, mix 71.2g 2-mercaptobenzimidazole with 128.2g 2-chloromethyl-3-methyl-4-(2,2,2-trifluoroethoxy base) pyridine hydrochloride into a three-necked flask. Start stirring and add 57g of sodium carbonate, then add 700ml of ethanol solution, heat to reflux for 1.5 hours, evaporate the solvent under reduced pressure, wash with water, and dry to obtain a white solid intermediate.

[0037] 2) Preparation of Lansoprazole: Add step (1) gained intermediate 130g in the there-necked flask of 1430ml chloroform, stir to make it dissolve, and cool the three-necked flask with ice-salt water bath, so that the temperature in the three-necked flask is...

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Abstract

The invention relates to the field of medicine production and in particular relates to a preparation method of a lansoprazole crystal type compound. The preparation method disclosed by the invention comprises the following steps of: by taking 2-mercapto benzimidazole and 2-chloromethyl-3-methyl-4-(2,2,2-trifluoroethoxy) pyridine hydrochloride as raw materials, carrying out condensation reaction and oxidation reaction, and refining to prepare the lansoprazole crystal. In the preparation process, the preparation condition is strictly controlled; the raw materials are low in cost and easy to purchase; the raw materials are reacted to finally generate the lansoprazole crystal type compound; 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 lansoprazole 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 short production period and further improving the production efficiency.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to a method for preparing a lansoprazole crystal compound. Background technique [0002] Ulcerative disease is a common type of disease, and it is prone to recurrent clinically, often accompanied by serious complications, such as gastric and duodenal ulcers, which may be complicated by upper gastrointestinal bleeding and perforation, which seriously threaten people's health. Proton pump inhibitors are powerful weapons in the fight against ulcer disease. [0003] Lansoprazole (Lansoprazole) is the second proton pump inhibitor anti-ulcer drug in the world developed by Takeda after Omeprazole (Omeprazole). This product is a new type of drug that inhibits gastric acid secretion, it acts on the H of gastric parietal cells ＋ -K ＋ -ATPase. H ＋ It cannot be transported to the stomach, so that the amount of gastric acid in the gastric juice is greatly reduced. It is clinically used f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
Inventor 李明杰李晓峰高菲菲刘延珍侯善波
Owner SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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