A kind of refining method and synthetic method of esomeprazole sodium

Abstract

The invention relates to a refining method and a synthesis method of esomeprazole. The refining method comprises the following steps: firstly, suspending a crude esomeprazole product in 2-5 times of good organic solvents, stirring at low temperature, filtering to remove the impurities, slowly adding 10-20 times of adverse organic solvents, stirring to crystallize over night, and centrifuging to dry, thereby obtaining a refined esomeprazole product. The refining method of the esomeprazole is stable and controllable in process, simple and convenient to operate and easy to industrialize; the prepared esomeprazole is hihg in purity, high in yield, high in optical purity and stable in component, and happening of adverse reaction accidents is greatly avoided.

Description

technical field

[0001] The invention relates to a preparation method of esomeprazole salt, in particular to a refining method of esomeprazole sodium and a synthesis method thereof. Background technique

[0002] Omeprazole, as the first proton pump inhibitor, has a history of more than ten years in the treatment of acid-related diseases. The drug has two optical isomers, a racemic mixture composed of S-omeprazole and R-omeprazole, of which S-omeprazole is also known as esomeprazole, which has an effect on gastric acid secretion. The inhibitory effect of omeprazole was significantly higher than that of single-dose administration of omeprazole.

[0003] Esomeprazole sodium (Esomeprazole sodium), S-omeprazole sodium, is a common esomeprazole salt, molecular formula: C 17 h 18 N 3 NaO 3 S, the appearance is white to light yellow powder, its chemical name is: 5-methoxy-2-((S)-((4-methoxy-3,5-dimethyl-2-pyridyl)methanol base) sulfinyl) -1H-benzimidazole sodium, its chemical s...

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