Vonoprazan fumarate polycrystalline forms and preparation method thereof

A technology of vonoprazan fumarate and crystal form, which is applied in the field of new crystal form of vonoprazan fumarate and its preparation, can solve the problems of few reports, achieve low cost, high product yield, and easy operation simple effect

Inactive Publication Date: 2016-02-10
NANJING HEALTHNICE MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] Vonorazan fumarate chemical name is 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethylamine Fumarate, there are few reports on the crystal form of Vonorazan fumarate

Method used

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  • Vonoprazan fumarate polycrystalline forms and preparation method thereof
  • Vonoprazan fumarate polycrystalline forms and preparation method thereof
  • Vonoprazan fumarate polycrystalline forms and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Preparation of Vonorazan Fumarate Form A

[0038] At room temperature, add 34.5g (0.1mol) of fumaric acid vonoprazan free base to a 1000ml single-necked bottle, add 345ml of ethyl acetate and stir evenly, add 11.6g (0.1mol) of fumaric acid to the above solution 116ml methanol solution, stirred and crystallized for one hour. After suction filtration, the filter cake was vacuum-dried at 50° C. to constant weight to obtain 38.0 g of vonoprazan fumaric acid crystal form A with a molar yield of 82.5%. It is characterized in that in the X-ray powder diffraction spectrum represented by Cu-Kα radiation and 2θ angle, there are characteristic diffraction peaks at 15.290, 20.403, 20.704, 21.572, 25.182, and 25.559, and the differential thermal analysis spectrum has an absorption peak at about 204.8°C.

[0039] The obtained solid X-ray diffraction is shown as figure 1 As shown, the differential thermal scanning calorimetry map is shown as figure 2 shown.

Embodiment 2

[0041] Preparation method 1 of vonorazan fumarate crystal form B

[0042] Add 46.1 g (0.1 mol) of vonoprazan fumaric acid crystal form A to a 2000 ml single-necked bottle, and add 922 ml of a mixed solution of methanol and water (ratio 1:1). Dissolve in a water bath at 50-60°C, stir and let cool to room temperature, and then filter with suction after stirring for 1 hour, and vacuum-dry the filter cake at 50°C to constant weight to obtain 36.8 g of vonoprazan fumaric acid Form B, with a molar yield of 79.8%. It is characterized in that in the X-ray powder diffraction spectrum represented by Cu-Kα radiation and 2θ angle, there are characteristic diffraction peaks at 12.253, 13.559, 15.259, 16.889, 17.422, 20.399, 20.764, 22.478, 25.198, 28.077, and the differential thermal analysis spectrum There is an absorption peak at about 209.0°C.

[0043] The obtained solid X-ray diffraction is shown as image 3 As shown, the differential thermal scanning calorimetry map is shown as Fi...

Embodiment 3

[0045] Preparation method 2 of vonorazan fumarate crystal form B

[0046] Add 46.1 g (0.1 mol) of vonoprazan fumaric acid crystal form A to a 2000 ml single-necked bottle, and add 922 ml of a mixed solution of ethanol and water (ratio 1:1). Dissolve in a water bath at 50-60°C, stir and let cool to room temperature, and then filter with suction after stirring for 1 hour, and vacuum-dry the filter cake at 50°C to constant weight to obtain 36.8 g of vonoprazan fumaric acid Form B, with a molar yield of 79.8%.

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Abstract

The invention discloses novel vonoprazan fumarate crystalline forms A and B and a preparation method suitable for industrial production. The prepared crystalline forms are simple in preparation technology, good in stability and capable of meeting the medicinal requirement.

Description

technical field [0001] The invention relates to a new crystal form of vonoprazan fumarate and a preparation method thereof. Background technique [0002] Vonoprazan fumarate is a new type of proton pump inhibitor, which can be used as an acid secretion inhibitor, a therapeutic drug for tumor diseases or autoimmune diseases. Omeprazole and the like can effectively inhibit gastric acid secretion as proton pump inhibitors, but the instability under acidic conditions and the dispersion of effects caused by metabolic enzyme polymorphisms and drug interactions (this is a known proton pump inhibitor Existing problems), vonoprazan fumarate has excellent stability under acidic conditions, so it shows better therapeutic effects on peptic ulcer, reflux esophagitis and the like. [0003] Vonorazan fumarate chemical name is 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethylamine Fumarate, there are few reports on the crystal form of vonoprazan fumarate. Con...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
CPCC07D401/12C07B2200/13
Inventor 赵思云蒋逸云张明雨王华娟
Owner NANJING HEALTHNICE MEDICAL TECH
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