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Vonoprazan fumarate new crystal form and preparation method thereof

A technology of vonorazan fumarate and its crystal form, which is applied in the field of medicine, can solve the problems of undiscovered polymorphs, etc., and achieve the effect of improving stability

Inactive Publication Date: 2017-03-08
海南欣莱医药科技股份有限公司
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  • Abstract
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Problems solved by technology

[0008] CN105315258A obtained two crystal forms by refining with ethyl acetate / methanol or alcohol / water, but it was mentioned in the pharmaceutical review report of Vonorazan fumarate that no polymorphism was found

Method used

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  • Vonoprazan fumarate new crystal form and preparation method thereof
  • Vonoprazan fumarate new crystal form and preparation method thereof
  • Vonoprazan fumarate new crystal form and preparation method thereof

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Embodiment

[0036] Preparation of new crystalline form and control crystalline form of vonoprazan fumarate

[0037] (1) Synthesis of Fumaric Acid Vonorazan Intermediate

[0038] Take 300g of 5-(2-fluorophenyl)-1H-pyrrole-3-carbaldehyde, 37.5g of 4-dimethylaminopyridine, 300g of N,N-diisopropylethylamine, and 1L of acetonitrile, and add them to the reaction flask. Dissolve 300 g of pyridine-3-sulfonyl chloride in 1 L of acetonitrile, and add it dropwise to the above reaction system at 20-30° C., and drop it in about 1 hour. After dropping, the temperature of the system was raised to 40-50°C, and the reaction was continued for 1 hour until the raw materials were completely consumed. The temperature of the system was lowered to 30° C., and 1.8 L of purified water was added dropwise to quench the reaction. The pH was adjusted to 4-5 with 0.5 mol / L HCl, and a yellow solid was precipitated. Add 3.6 L of purified water to the system, and stir at 0-10°C for 1 hour. After suction filtration, th...

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Abstract

The invention discloses a vonoprazan fumarate new crystal form and a preparation method thereof. The preparation method comprises the following step: taking ethyl acetate, methanol and purified water as a mixed crystallizing solvent to obtain the vonoprazan fumarate new crystal form; and in a powder X-ray diffraction map of the vonoprazan fumarate new crystal form, characteristic peaks exist in positions where diffraction angles 2 theta are 12.18+ / - 0.5, 13.43+ / - 0.5, 22.35+ / - 0.5, 37.06+ / - 0.5 and 38.25+ / - 0.5. The vonoprazan fumarate new crystal form is good in stability; addition of medicine impurities can be avoided effectively; high costs caused by storage are reduced; and an effective guarantee is provided for safety of products and clinical effects.

Description

[0001] field of invention [0002] The invention relates to the technical field of medicine, in particular to a new crystal form of vonoprazan fumarate and a preparation method thereof. Background technique [0003] Vonoprazan fumarate (TAK-438), chemical name 1-[5-(2-fluorophenyl)-1-(pyridine-3-sulfonyl)-1H-pyrrol-3-yl ]-N-methylmethylamine monofumarate is a new type of potassium ion channel blocker developed by Takeda Pharmaceutical Company of Japan. It was launched in Japan in 2015 and is used for the treatment of non-erosive gastroesophageal reflux disease, Duodenal ulcer, gastric ulcer, erosive esophagitis, etc. The chemical structural formula is shown in (1). [0004] [0005] Vonoprazan fumarate inhibits basal gastric acid secretion in a concentration-dependent manner, ID 50 The value is 1.26 mg / kg. In animal experiments compared with lansoprazole, vonoprazan fumarate has a stronger inhibitory effect on gastric acid secretion, a faster increase in the pH value of...

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 邝少轶陈年根王印云晓
Owner 海南欣莱医药科技股份有限公司
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