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Lansoprazole crystal compound

A technology for lansoprazole crystals and compounds, which is applied in the field of anti-ulcer drugs, can solve the problems of high price and high cost of raw materials, and achieve the effects of low cost, low recurrence rate and rapid ulcer treatment

Active Publication Date: 2013-08-21
SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD +2
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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

[0026] The present embodiment provides a lansoprazole crystal form compound, its character is crystal form, chemical name is: 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)- 2-pyridyl]methyl]sulfinyl]-1H-benzimidazole, chemical name: C 16 h 14 f 3 N 3 o 2 S, the molecular formula is:

[0027]

[0028] Its preparation method is to use 2-mercaptobenzimidazole as raw material, undergo condensation and oxidation reactions, and then refine it. The specific preparation process is as follows:

[0029] 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%. ...

Embodiment 2

[0069] The difference from Example 1 is that the preparation method of lansoprazole crystal form compound uses 2-mercaptobenzimidazole as a raw material, undergoes condensation and oxidation reactions, and is then refined. The specific preparation process is as follows:

[0070] 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.

[0071] 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 wa...

Embodiment 3

[0075] The difference from Example 1 is that the preparation method of lansoprazole crystal form compound uses 2-mercaptobenzimidazole as a raw material, undergoes condensation and oxidation reactions, and is then refined. The specific preparation process is as follows:

[0076] 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.

[0077] 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-nec...

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Abstract

The invention relates to the field of anti-ulcer medicines, and in particular relates to a lansoprazole crystal compound. The character of the lansoprazole crystal compound is crystal; the chemical name of the lansoprazole crystal compound is 2-[[[3-methyl-4-(2,2,2-trifluoroethoxyl)-2-pyridyl] methyl] sulfinyl]-1H-benzimidazole, namely C16H14F3N3O2S; according to a mass spectrum, the molecule ion peak of the product is [M+H]<+>; and the mass-to-charge ratio m / z is 370. The preparation method comprises the following steps of: performing a condensation reaction and an oxidation reaction, and then performing refining. According to the lansoprazole crystal compound, proper raw materials are adopted, and the cost is low; the crystal compound has extremely good treating effects for ulcer diseases such as gastric ulcer, duodenal ulcer, refractory ulcer, reflux esophagitis and pancreatic original ulcer after being taken properly; an experiment shows that the lansoprazole crystal compound is basically non-toxic, can treat the ulcer in a more quick and effective manner and is low in recurrence rate; through repeated experimental selection, the defined preparation method is simple and feasible; the selected raw materials are readily available; and the cost is low.

Description

technical field [0001] The invention relates to the field of anti-ulcer drugs, in particular to a crystal compound of lansoprazole. 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 for duodenal ulcer, gastr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12A61P1/04
Inventor 李明杰刘明霞曹传张明法张继文
Owner SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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