Preparation method of low-impurity Vonoprazan fumarate

A technology of vonorazan fumarate and impurities, applied in the field of medicine, can solve the problems of difficult realization, unrealistic feeding weight, low yield, etc., and achieve the effects of prolonging the process cycle, saving energy, and reducing the introduction of organic solvents
CN110590746APending Publication Date: 2019-12-20JILIN HUIKANG PHARM CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
JILIN HUIKANG PHARM CO LTD
Publication Date
2019-12-20

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Abstract

The invention provides a preparation method of low-impurity Vonoprazan fumarate. A method for removing impurities A-E during preparation of Vonoprazan comprises the steps: preparing Vonoprazan hydrobromide from Vonorazan, and removing the impurities A-E which are difficult to remove by using a recrystallization purifying method, wherein the method for removing the impurities A-E during preparationof Vonoprazan has good selectivity to the impurities A-E. The preparation method of low-impurity Vonoprazan fumarate comprises the steps: performing a reaction on 5-(2-fluorophenyl)-1-(pyridyl-3-ylsulfonyl)-1H-pyrrole-3-formaldehyde and methylamine or a salt of methylamine, then performing reduction so as to obtain Vonoprazan, then preparing Vonoprazan hydrobromide, then performing salt dissociation so as to obtain Vonoprazan free alkali, preparing Vonoprazan fumarate with a purity of 99.7% or above, and then performing recrystallization refining so as to obtain Vonoprazan fumarate with a purity of 99.9% or above. The invention provides an impurity D, a preparation method of the impurity D and application of the impurity D as an impurity reference substance in Vonoprazan fumarate.
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Description

Technical field

[0001] The invention relates to the technical field of medicine, in particular to a preparation method of low-impurity fumarate voronolazan. Background technique

[0002] Voronolazan fumarate was developed by Takeda Pharmaceutical Co., Ltd., and is mainly used to treat gastric ulcer, duodenal ulcer, reflux esophagitis, and inhibit the recurrence of gastric ulcer or duodenal ulcer. Voronolazan fumarate is a novel potassium ion (K + ) Competitive acid blocker (P-CAB), which can inhibit K in the last step of gastric acid secretion by parietal cells + Right H + -K + -The combination of ATPase (proton pump) stops the secretion of gastric acid in advance, and has a strong and long-lasting effect of inhibiting gastric acid secretion.

[0003] Chinese patent application CN102421753A discloses that 5-(2-fluorophenyl)-1H-pyrrole-3-carbaldehyde is used as a raw material and reacted with pyridine-3-sulfonyl chloride to obtain intermediate 5-(2-fluorophenyl)-1 -(Pyridin-3-ylsul...

Claims

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