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Novel esomeprazole compound entity as well as preparation method and combined pharmaceutical preparation thereof

A new technology for esomeprazole and omeprazole, applied in the field of medicine, can solve the problems of restricting the use of esomeprazole, prone to toxic side effects, low utilization rate and the like, and achieves good shape and is not easy to degrade. , the effect of less impurities

Inactive Publication Date: 2015-04-29
ZHEJIANG CHANGDIAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The current esomeprazole has problems such as low purity, many impurities, poor stability, low yield, prone to toxic and side effects, and prone to degradation and discoloration, which limits the use of esomeprazole
[0006] The existing omeprazole freeze-dried preparations have problems such as poor effect, low utilization rate, poor stability, and prone to toxic and side effects

Method used

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  • Novel esomeprazole compound entity as well as preparation method and combined pharmaceutical preparation thereof
  • Novel esomeprazole compound entity as well as preparation method and combined pharmaceutical preparation thereof
  • Novel esomeprazole compound entity as well as preparation method and combined pharmaceutical preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] A new compound entity of esomeprazole, its chemical structural formula is

[0031]

[0032]The new esomeprazole compound entity is determined by X-ray powder diffraction, and its spectrum has the following diffraction angle 2θ, with an error of ±0.2°, expressed in angles as 5.8°, 10.0°, 11.5°, 12.6°, 16.2°, 17.0°, 18.9°, 20.9°, 21.5°, 22.2°, 23.1°, 25.8°, 26.4°; the corresponding D values ​​are 15.32, 8.887, 7.724, 7.062, 5.493, 5.234, 4.715,

[0033] 4.288, 4.164, 4.031, 3.877, 3.473, 3.395.

[0034] The preparation method of above-mentioned esomeprazole novel compound entity, the method comprises the steps:

[0035] Add 360 grams of 5-methoxy-2-mercapto-1H-benzimidazole and 444 grams of 2-chloromethyl-3,5-dimethyl-4-methoxypyridine hydrochloride in the reactor, and then Add 3600 grams (4547ml) of anhydrous methanol, and heat to reflux to clarify the solution. Then add 1257 grams of 14% sodium hydroxide solution, heat and reflux for 4 hours, after the reaction is...

Embodiment 2

[0042] A new compound entity of esomeprazole, its chemical structural formula and X-diffraction powder diffraction pattern are as in Example 1.

[0043] The preparation method of above-mentioned esomeprazole novel compound entity, the method comprises the steps:

[0044] Add 360 grams of 5-methoxy-2-mercapto-1H-benzimidazole and 444 grams of 2-chloromethyl-3,5-dimethyl-4-methoxypyridine hydrochloride in the reactor, and then Add 3780 grams (4774ml) of anhydrous methanol and heat to reflux to clarify the solution. Then add 1227 grams of 15% sodium hydroxide solution, heat and reflux for 3.8 hours, after the reaction is complete, adjust the pH value to 6-7 with concentrated hydrochloric acid, filter, concentrate under reduced pressure to completely recover the solvent methanol, and use 25.5 kg of dichloromethane (19.2L) was dissolved by heating under reflux with stirring, washed three times with 4500ml of saturated brine, dried with anhydrous sodium sulfate for 2 hours, filtere...

Embodiment 3

[0051] A new compound entity of esomeprazole, its chemical structural formula and X-diffraction powder diffraction pattern are as in Example 1.

[0052] The preparation method of above-mentioned esomeprazole novel compound entity, the method comprises the steps:

[0053] Add 360 grams of 5-methoxy-2-mercapto-1H-benzimidazole and 444 grams of 2-chloromethyl-3,5-dimethyl-4-methoxypyridine hydrochloride in the reactor, and then Add 3960 grams (5000 ml) of anhydrous methanol, and heat to reflux to clarify the solution. Then add 1200 grams of 16% sodium hydroxide solution, heat and reflux for 3.5 hours, after the reaction is complete, adjust the pH value to 6-7 with concentrated hydrochloric acid, filter, concentrate under reduced pressure to completely recover the solvent methanol, and use 26.6 kg of dichloromethane (20L) heated to reflux and stirred to dissolve, washed three times with 5000ml of saturated brine, dried with anhydrous sodium sulfate for 2 hours, filtered, concentr...

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Abstract

The invention discloses a novel esomeprazole compound entity as well as a preparation method and a combined pharmaceutical preparation thereof. The novel esomeprazole compound entity is measured by adopting X-ray powder diffraction, the map sequentially has the following diffraction angles 2theta: 5.8 degrees, 10.0 degrees, 11.5 degrees, 12.6 degrees, 16.2 degrees, 17.0 degrees, 18.9 degrees, 20.9 degrees, 21.5 degrees, 22.2 degrees, 23.1 degrees, 25.8 degrees and 26.4 degrees, the error of each angle is + / -0.2 degrees, and the corresponding D values sequentially refer to 15.32, 8.887, 7.724, 7.062, 5.493, 5.234, 4.715, 4.288, 4.164, 4.031, 3.877, 3.473 and 3.395. The novel esomeprazole compound entity disclosed by the invention has the advantages of high purity, few impurities, high yield, high stability, few toxic and side effects and the like.

Description

technical field [0001] The invention relates to a new esomeprazole compound entity, a preparation method thereof and a drug combination preparation, belonging to the technical field of medicine. Background technique [0002] Omeprazole, its chemical name is: 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)-methyl]-sulfinyl]- 1H-benzimidazole, molecular formula: C 17 h 19 N 3 o 3 S, molecular weight: 345.42. [0003] Omeprazole is a proton pump inhibitor that can effectively inhibit the secretion of gastric acid. It also has an inhibitory effect on pepsin secretion, does not significantly change gastric mucosal blood flow, and does not affect body temperature, gastric cavity temperature, arterial blood pressure, venous hemoglobin, arterial oxygen partial pressure, carbon dioxide partial pressure, and arterial blood pH. It is also effective for gastric and duodenal ulcers, reflux or erosive esophagitis, and Zoe-Ehrlich syndrome, etc. It is also effective for gastric and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12A61K31/4439A61P1/04
CPCC07D401/12
Inventor 陈宇东厉达中来杭佳胡国胜
Owner ZHEJIANG CHANGDIAN PHARMA
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