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Method for preparing esomeprazole sodium

A technology of esomeprazole sodium and omeprazole sulfide, which is applied in the field of drug synthesis, and achieves the effects of simple method, improved efficiency and stable combination

Inactive Publication Date: 2016-04-20
QINGDAO CHENDA BIOLOGICAL SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The object of the present invention is to overcome the defect of the preparation method of existing esomeprazole salt, provide a kind of preparation method of the esomeprazole sodium that yield is high, selectivity is good and reaction efficiency height is suitable for industrial scale production

Method used

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  • Method for preparing esomeprazole sodium
  • Method for preparing esomeprazole sodium

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] A preparation method of esomeprazole sodium, comprising the following steps:

[0026] 1) Mix 630g (2mol) of omeprazole sulfide with the compound represented by formula M and inorganic metal salt in 5L of acetone, the mixing conditions are: temperature 55°C, stirring for 1 hour to obtain mixture A; wherein, The molar ratio of omeprazole sulfide to the compound represented by formula M and the inorganic metal salt is 1:0.6:0.2, and the inorganic metal salt is CoCl 2 .

[0027] 2) At a temperature of 50°C, 30% H 2 o 2 Drop into step 1) in the mixture A and carry out oxidation reaction, add sodium hydroxide methanol solution after reaction finishes, obtain esomeprazole sodium; 2 o 2 Gauge, 30%H 2 o 2 The molar ratio to omeprazole thioether is 2; the amount of sodium hydroxide methanol solution added, calculated as sodium hydroxide, has a molar ratio to omeprazole thioether of 1.6.

[0028] 3) the obtained esomeprazole sodium is carried out the process of refinement, ...

Embodiment 2

[0030] A preparation method of esomeprazole sodium, comprising the following steps:

[0031] 1) Mix 630 g (2 mol) of omeprazole sulfide with the compound represented by formula M and inorganic metal salt in 5 L of acetone, the mixing conditions are: temperature 50 ° C, stirring for 0.5 hours, to obtain mixture A; wherein, The molar ratio of omeprazole sulfide to the compound represented by formula M and the inorganic metal salt is 1:0.55:0.1, and the inorganic metal salt is CoSO 4 .

[0032] 2) At a temperature of 45°C, 30% H 2 o 2 Drop into step 1) in the mixture A and carry out oxidation reaction, add sodium hydroxide methanol solution after reaction finishes, obtain esomeprazole sodium; 2 o 2 Gauge, 30%H2 o 2 The molar ratio to omeprazole thioether is 1.8; the amount of sodium hydroxide methanol solution added, calculated as sodium hydroxide, is 1.6 to the molar ratio of omeprazole thioether.

[0033] 3) The process of refining the obtained esomeprazole sodium, the re...

Embodiment 3

[0035] A preparation method of esomeprazole sodium, comprising the following steps:

[0036] 1) Mix 630 g (2 mol) of omeprazole sulfide with the compound represented by formula M and inorganic metal salt in 5 L of acetone, the mixing conditions are: temperature 45 ° C, stirring for 1 hour, to obtain a mixture A; wherein, The molar ratio of omeprazole sulfide to the compound represented by formula M and the inorganic metal salt is 1:0.5:0.15, and the inorganic metal salt is CoCl 2 .

[0037] 2) At a temperature of 50°C, 30% H 2 o 2 Drop into step 1) in the mixture A and carry out oxidation reaction, add sodium hydroxide methanol solution after reaction finishes, obtain esomeprazole sodium; 2 o 2 Gauge, 30%H 2 o 2 The molar ratio to omeprazole thioether is 1.4; the amount of sodium hydroxide methanol solution added, calculated as sodium hydroxide, is 1.8 to the molar ratio of omeprazole thioether.

[0038] 3) The obtained esomeprazole sodium is carried out the process of ...

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Abstract

The invention discloses a method for preparing esomeprazole sodium. The method comprises the following steps: (1) mixing Omeprazole sulfide prepared in the step (1) with a compound as shown in a formula M and inorganic metal salts in acetone to obtain a mixture A; (2) dripping 30% H2O2 into the mixture A prepared in the step (1) at a temperature of 10-50 DEG C to conduct an oxidation reaction, and adding a sodium hydroxide methanol solution after the reaction is completed to obtain esomeprazole sodium, wherein in the step (1), the inorganic metal salt is cobalt (II), iron (II) or manganese (II) metal salt. The method has the advantages of high yield, good selectivity and high reaction efficiency, and is suitable for industrial large-scale production.

Description

technical field [0001] The invention belongs to the field of drug synthesis, in particular to a preparation method of esomeprazole sodium. Background technique [0002] Esomeprazole, 5-methoxy-2-[(S)-(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]benzene-1H-benzene Omeprazole, the world's first proton pump inhibitor, is the S-optical isomer of omeprazole, which can reduce gastric acid secretion by inhibiting the proton pump of gastric parietal cells. Esomeprazole sodium is the sodium salt of esomeprazole. [0003] At present, esomeprazole salt is mainly obtained by esomeprazole salification, therefore, the preparation method of esomeprazole not only affects the yield and the purity of esomeprazole, but also affects the yield and purity of esomeprazole salt. yield and purity. The methods commonly used in the preparation of esomeprazole include: resolution of racemic omeprazole, asymmetric catalytic oxidation of omeprazole sulfide and biochemical oxidation. The racemic...

Claims

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Application Information

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IPC IPC(8): C07D401/12
CPCC07D401/12
Inventor 陈令浩
Owner QINGDAO CHENDA BIOLOGICAL SCI & TECH
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