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Refining method of lesinurad

A refining method and high-quality technology, applied in the field of medicine, can solve the problems of tediousness and incompatibility with the requirements of industrialized large-scale production, and achieve the effects of easy drying and shortening of drying time.

Pending Publication Date: 2019-07-05
XUZHOU WANBANG JINQIAO PHARMA +1
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In the synthetic routes that have been reported in patent literature, for the refining steps of each step of intermediates and finished products, some procedures are cumbersome to operate, and there are defects such as not being suitable for industrialized large-scale production.

Method used

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  • Refining method of lesinurad
  • Refining method of lesinurad
  • Refining method of lesinurad

Examples

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Embodiment 1

[0036] 1) Add 400ml of the reaction solvent DMF to a 1000ml three-necked reaction flask, and then add 100g of starting material 4-(4-cyclopropylnaphthalene-1-yl)-1H-1,2,4-tri Azole-5(4H)-thiol was stirred and dissolved at 15-20°C to obtain A solution. Add 39.7g of powdered anhydrous sodium carbonate to solution A, and add 65.7g of ethyl bromoacetate dropwise at 10-15°C to control the rate of addition. During the dropping process, the internal temperature does not exceed 15°C. The internal temperature was 10-15°C, and the reaction was carried out with heat preservation. After thin-layer chromatography, the reaction of the raw materials was complete, and the reaction was stopped after extending the reaction for 15 minutes.

[0037] Transfer the reaction solution to a 5L beaker, add 1.2L of purified water at 0-5°C dropwise to the system at an internal temperature of 0-5°C, a large amount of precipitation occurs, continue to stir at 0-5°C for 0.5h, and filter with suction. When a...

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Abstract

The invention discloses a synthetic refining method of lesinurad. The method includes: taking 4-(4-cyclopropyinaphthalene-1-yl)-1H-1, 2, 4-triazole-5(4H)-mercaptan as the starting raw material, carrying out alkylation reaction with ethyl bromoacetate, bromination reaction with N-bromosuccinimide, sodium hydroxide hydrolysis, hydrobromic acid neutralization, refining and drying to successfully synthesize a high purity lesinurad bulk drug finished product, and purifying the intermediates of all steps and the product, thus obtaining the high purity final product meeting the requirements. The method provided by the invention is easy for product collection, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a method for refining Resinard. Background technique [0002] Recinard, molecular formula: C 17 h 14 BrN 3 o 2 S, its Chinese name: 2-((5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl)thio)acetic acid, Product name: Zurampic, its structural formula is: [0003] [0004] Resinard is developed by AstraZeneca and the world's first marketed urate reabsorption transporter (URATI) inhibitor. At the end of 2015 and early 2016, respectively, it was approved by the US FDA and the EU EMA for the treatment of gout associated with hyperuricemia in combination with a xanthine oxidase inhibitor (XOI); , to apply for clinical application, so far no domestic manufacturers have applied for it, and it belongs to category 3.1 generic drugs. [0005] The patent application for the drug involves many aspects such as synthesis process, crystal form, crystal form ...

Claims

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Application Information

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IPC IPC(8): C07D249/12
CPCC07D249/12
Inventor 吴增乔德水高雪芹
Owner XUZHOU WANBANG JINQIAO PHARMA
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