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Vonoprazan purification method

A purification method, monohydric alcohol technology, applied in the direction of organic chemistry, etc., can solve the problems affecting the purity of vonoprazan raw material medicine, and achieve the effect of mild conditions and simple operation

Active Publication Date: 2020-04-17
ZHUZHOU QIANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, it has been found in practice that the methylamine reagent used in the reaction will inevitably have impurity dimethylamine, which will cause the synthesized product Vonorazan to contain an impurity compound I similar to its structure, which will affect the quality of the Vonorazan bulk drug. purity, and there is no impurity removal and purification method for impurity compound I in the prior art

Method used

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Embodiment 1

[0035] Embodiment 1 Purification of Vonorazan Crude Product

[0036] The crude product of Vonorazan was purified as follows:

[0037] Add 10g of Vonorazan crude product into the refining solvent, the addition amount of the refining solvent is 10mL / g, stir and dissolve at 65°C for 10min, first cool down to 25°C to precipitate the solid, keep it warm for 30min, then cool down to 4°C to continue crystallization After 60 minutes, suction filtration, the solid was washed with a mixed solution prepared by monohydric alcohol and water at a volume ratio of 7:3, the amount of the washing solution added was 2mL / g, and after drying under reduced pressure at 50°C, the refined product of Devonorazan .

[0038] Determination of the purity of Vonorazan refined product and the content of impurity compound I. Refer to Table 1 for the specific refining solvent ratio and the purity of the obtained Vonorazan refined product and the content of impurity compound I.

[0039] Table 1 Vonorazan pur...

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Abstract

The invention discloses a purification method of vonoprazan. The method comprises the following steps: preparing a refined solvent from a monohydric alcohol, formamide and water according to a certainratio; and purifying a vonoprazan crude product under the gradient cooling condition, so that an impurity compound I existing in vonoprazan can be remarkably removed, high yield is kept while the purity of vonoprazan is improved, and the method is easy to operate, mild in condition, beneficial to subsequent preparation of vonoprazan fumarate and suitable for large-scale industrial production.

Description

technical field [0001] The invention belongs to the technical field of chemical synthesis. More specifically, it relates to a purification method of Vonorazan. Background technique [0002] Vonorazan fumarate is a new type of gastric acid secretion inhibitor (potassium ion competitive acid blocker, P-CAB), which has the characteristics of fast onset, strong and long-lasting acid suppression effect, and can be used to treat Helicobacter pylori Infection, gastroesophageal reflux, peptic ulcer, duodenal ulcer, esophagitis, gastric ulcer and other acid-related diseases (ARDs). And the results of in vitro experiments show that compared with lansoprazole, vonoprazan fumarate has 400 times the ability to inhibit the proton pump. + 、K + - The selectivity of ATPase is more than 500 times; in animal experiments, vonoprazan fumarate showed a higher enrichment rate and slower clearance rate than lansoprazole, which makes it have a stronger in vivo Potency and longer-lasting acid sup...

Claims

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Application Information

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IPC IPC(8): C07D401/12
CPCC07D401/12
Inventor 金秉德宿亮郭伟邹斌彬龚翠云李翼
Owner ZHUZHOU QIANJIN PHARMA