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Refining method of topiroxostat

A refining method, the technology of topirastat, applied in the direction of organic chemistry, etc., can solve the problem of less research on the refining method of topirastat, and achieve the effect of improving the refining effect

Inactive Publication Date: 2018-03-09
TIANJIN HANRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In the prior art, CN1561340 and CN105348264A all disclose the preparation method of topirastat, but there is less research on the refined method with topirastat, and it is still necessary to develop a kind of process that is simple, easy to operate, low in production cost and high in product quality. Method for refining topirastat with high purity, stable process and suitable for industrial production

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Put 20g of topirastat crude product, 90ml of ethyl acetate and 10ml of isopropanol into the reaction flask, raise the temperature to 40°C, all the solids are dissolved, add 0.5g of activated carbon, reflux for 20min, keep warm at 40°C and filter, collect the filtrate. The filtrate was reheated to reflux, stopped heating and cooled down to 0°C, stirred and crystallized for 12 hours, filtered, washed the filter cake with 50ml of n-hexane, and dried in vacuum at 40°C for 12 hours to obtain 18.9g of topirastat fine product.

Embodiment 2

[0024] Put 20g of topirastat crude product, 180ml of ethyl acetate and 20ml of isopropanol into the reaction flask, raise the temperature to 42°C, all the solids are dissolved, add 0.5g of activated carbon, reflux for 30min, heat-preserve and filter, and collect the filtrate. The filtrate was reheated to reflux, stopped heating and cooled to 0°C, stirred and crystallized for 12 hours, filtered, the filter cake was washed with 50ml of n-hexane, and vacuum-dried at 60°C for 12 hours to obtain 18.1g topirastat fine product.

Embodiment 3

[0026] Put 20g of crude topirastat, 150ml of ethyl acetate and 10ml of tert-butanol into the reaction flask, raise the temperature to 40°C, all the solids are dissolved, add 0.5g of activated carbon, reflux for 1h, keep at 40°C and filter, and collect the filtrate. The filtrate was reheated to reflux, stopped heating and cooled to 0°C, stirred and crystallized for 12 hours, filtered, the filter cake was washed with 50ml of n-heptane, and vacuum-dried at 40°C for 12 hours to obtain 18.3g topirastat fine product.

[0027] Table 1 Topirastat refining effect data comparison

[0028]

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PUM

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Abstract

The invention belongs to the field of drug synthesis and relates to a method for refining high-purity topirastat. The refining method of topirastat according to the present invention comprises the following steps: adding topirastat crude product into an organic solvent, heating and stirring until completely dissolved, activated carbon decolorization, natural cooling and crystallization, filtering and drying to obtain high-purity topirastat Stata. The refined method of the invention has simple process, convenient operation, low production cost, high product purity, stable process and is suitable for industrialized production.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and in particular relates to a method for refining topirastat. Background technique [0002] Topiroxostat (Topiroxostat), the chemical name is 5-(2-cyano-4-pyridyl)-3-(4-pyridyl)-1,2,4-triazole, which is produced by Japan Fuji Pharmaceutical Co., Ltd. A new molecular entity drug developed and launched for the first time in Japan in August 2013 for the treatment of gout and hyperuricemia. [0003] In the prior art, CN1561340 and CN105348264A all disclose the preparation method of topirastat, but there is less research on the refined method with topirastat, and it is still necessary to develop a kind of process that is simple, easy to operate, low in production cost and high in product quality. A method for refining topirastat with high purity, stable process and suitable for industrial production. Contents of the invention [0004] Aiming at the deficiencies of the prior art, the present inventio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/14
CPCC07D401/14
Inventor 严洁
Owner TIANJIN HANRUI PHARMA
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