Method for synthesizing and refining esomeprazole sodium

Abstract

The invention relates to a method for synthesizing and refining esomeprazole sodium. The method comprises the following several steps: (1) carrying out condensation by taking 2-sulfydryl-5-methoxybenzimidazole and 2-chloromethyl-3.5-dimethyl-4-methoxypyridine hydrochloride as raw materials to generate prochiral thioether; (2) synthesizing the prochiral thioether into an esomeprazole crude product under the action of D-(-) diethyl tartrate, water, tetraisopropyl titanate, diisopropylethylamine and cumene hydroperoxide, and refining to generate esomeprazole potassium salt; (3) dissolving the esomeprazole potassium salt, then transforming into esomeprazole sodium salt, and refining to obtain a final product. The process of the esomeprazole sodium has the advantages of easiness for operation, good reaction repeatability and higher yield; the obtained product is high in purity and suitable for industrialized production.

Description

technical field

[0001] The invention relates to a production synthesis and refining process of esomeprazole sodium, which belongs to the technical field of medicine. Background technique

[0002] Chemical name of esomeprazole sodium: 5-methoxy-2-((S)-((4-methoxy-3,5-dimethyl-2-pyridyl)methyl)sulfinyl -1H-Benzimidazole Sodium

[0003] The structural formula is:

[0004]

[0005] Molecular formula: C 17 h 18 N 3 NaO 3 S

[0006] Molecular weight: 367.41

[0007] Esomeprazole sodium is the levoisomer of omeprazole sodium, which was developed by AstraZeneca and first launched in the United States in 1999. It is the first isomer proton pump inhibitor (PPI) to be marketed. Esomeprazole sodium reduces gastric acid secretion by specifically inhibiting the proton pump of gastric parietal cells, so it can effectively treat gastric ulcer, duodenal ulcer, functional dyspepsia and reflux esophagitis and other diseases. Compared with omeprazole sodium, esomeprazole sodium meta...

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