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Method for preparing esomeprazole magnesium

A technology for esomeprazole magnesium and esomeprazole, which is applied in the field of chemical preparation, can solve the problems of long production cycle, environmental pollution, difficult operation and the like, achieves shortened production cycle, improved yield and purity, and can be used volume reduction effect

Inactive Publication Date: 2015-12-16
INST OF PHARMACY SHANDONG PROV ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the synthesis routes of esomeprazole magnesium in the existing reports all have shortcomings such as long production cycle, high cost, difficult operation, and serious environmental pollution, wherein the low yield is the most serious problem, and the molar yield is mostly less than 80 %, the molar yield of some technological routes is only about 50%

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Add 3.6g (0.15mol) of magnesium powder, 42.0g (0.12mol) of esomeprazole and 5ml (0.078mol) of dichloromethane into 300ml of methanol, select different ultrasonic frequencies, microwave frequency 2450MHz, in ultrasonic microwave Under synergistic effect, heat to 40-45°C, stir for 1 hour, and filter. The filtrate was distilled to dryness under reduced pressure at 35°C. Add 400ml of acetone and stir at 30°C for 1 hour. Suction filtration, washing with a small amount of acetone. Dissolve the obtained solid in 200ml of methanol, add 10ml of water, stir at 30°C for 0.5 hours, then pour the reaction solution into 1000ml of ice water (about 0-1°C), stir for 1 hour, filter with suction, and wash with 300ml of water . drying.

[0020] .

Embodiment 2

[0022] Add 72g (3.00mol) of magnesium powder, 100ml (1.56mol) of dichloromethane and 840.0g (2.4mol) of esomeprazole to 5L of methanol, select an ultrasonic frequency of 25KHz, select a different microwave frequency, and Under synergistic effect, heat to 45°C, stir for 2h, and filter. The filtrate was distilled to dryness under reduced pressure at 35°C. Add 5 L of acetone and stir at 35°C for 2 hours. Suction filtration, washing with a small amount of acetone. Dissolve the obtained solid in 3L of methanol, add 200ml of water, stir at 25-35°C for 1 hour, then pour the reaction solution into 15L of ice water, stir for 2 hours, filter with suction, and wash with 5L of water. drying. .

Embodiment 3

[0027] Add 3.5g (0.15mol) of magnesium powder, 5ml (0.078mol) of dichloromethane and 42.0g (0.12mol) of esomeprazole into 280ml of methanol, select the ultrasonic frequency of 25KHz, and the microwave frequency of 2450MHz. Under the action, heated to 45°C and stirred for 1h, and filtered. The filtrate was distilled to dryness under reduced pressure at 35°C. Add 400ml of organic solvent and stir at 30°C for 1 hour. Suction filtration, and then wash with a small amount of the same organic solution. The obtained solid was dissolved in 200ml of methanol, 10ml of water was added, and stirred at 30°C for 0.5 hour, then the reaction solution was poured into 1000ml of ice water, stirred for 1 hour, suction filtered, and washed with 300ml of water. drying.

[0028] .

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Abstract

The invention provides a method for preparing esomeprazole magnesium. The method comprises the following steps: enabling esomeprazole and magnesium powder to react in absolute methanol under the synergistic effect of ultrasonic microwaves, filtering the obtained salt forming reaction liquid, performing vacuum concentration, adding an organic solvent for washing, further washing with water, and drying, thereby obtaining an esomeprazole magnesium product. When esomeprazole magnesium is prepared by using the method, a strict anhydrous condition is not needed in salt forming reaction, the production period is greatly shortened, the operation is simple, the salt forming reaction is complete, and the yield can be 87-95%; and more importantly, the methanol and organic solvent used in the reaction process can be recycled and applied mechanically, so that the production cost is lowered, and relatively high environmental-friendly values can be achieved. In addition, the esomeprazole magnesium product prepared by using the method provided by the invention is relatively high in purity, and the quality can be relatively easy to control.

Description

technical field [0001] The invention relates to the field of chemical medicine preparation, in particular to a preparation method of esomeprazole magnesium. Background technique [0002] Esomeprazole magnesium is the S-optical isomer of omeprazole, which is a proton pump inhibitor. It can reduce gastric acid secretion by inhibiting the H+ / K+-ATPase of gastric parietal cells, prevent the formation of gastric acid, and treat peptic Acid-related diseases such as ulcers and gastroesophageal reflux disease. It is the first optically pure proton pump inhibitor on the market. Its sodium salt can be used as an injection preparation and was launched in Europe in 2003; its magnesium salt can be used as an oral preparation and was launched in Europe in 2000. Compared with omeprazole, it has a strong and long-lasting acid inhibitory effect, and the percentage of time when the pH of gastric juice is greater than 4 within 24 hours is 50% (34% for omeprazole), and it also has a certain pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
CPCC07D401/12
Inventor 孙捷姚庆强汪海洋
Owner INST OF PHARMACY SHANDONG PROV ACAD OF MEDICAL SCI
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