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Crystal form and preparation of febuxostat

A crystal form, isobutoxyphenyl technology, applied in the chemical field, can solve problems such as the crystal form not described, and achieve the effects of not easy crystal transformation, safe production and preparation process, and good dissolution rate

Active Publication Date: 2009-04-22
SHANGHAI INST OF PHARMA IND +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] EP 513379 reports the synthesis method of febuxostat, which mentions recrystallization with ethanol to obtain the final product, but does not describe the crystal form

Method used

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  • Crystal form and preparation of febuxostat
  • Crystal form and preparation of febuxostat
  • Crystal form and preparation of febuxostat

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] The preparation method of febuxostat crystal form:

[0025] Add 10 g of febuxostat to 200 ml of ethyl acetate, heat to 78°C to dissolve, then cool to room temperature while stirring, and filter after 2 hours. Dry at 60°C. 8.5 g of crystal form III sample was obtained. The melting point is 209-210°C.

Embodiment 2

[0027] The preparation method of febuxostat crystal form:

[0028] Add 10 g of febuxostat to 300 ml of ethyl acetate and heat to 60°C to dissolve, then cool to room temperature while stirring, and filter after 2 hours. Dry at 60°C. A 7.9 g sample of crystal form III was obtained. The melting point is 208-209°C.

Embodiment 3

[0030] The preparation method of febuxostat crystal form:

[0031] Add 10 g of febuxostat to 250 ml of ethyl acetate and heat to 60°C to dissolve, then cool to room temperature while stirring, and filter after 2 hours. Dry at 60°C. A 8.2 g sample of crystal form III was obtained.

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PUM

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Abstract

The invention provides a crystal form of anti-hyperuricemia drug 2-(3-cyano-4-isooxyphenyl)-4-methyl-5-thiazole formic acid and a method for preparing the same. The method for preparing the crystal form mainly comprises the following steps: heating up and dissolving the 2-(3-cyano-4-isooxyphenyl)-4-methyl-5-thiazole formic acid in ethyl acetate, and cooling down the solution for recrystallizing the solution to obtain the crystal form. The crystal form has better dissolution degree and stability.

Description

technical field [0001] The invention relates to the field of chemistry, in particular to a crystal form of 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid and a preparation method thereof. Background technique [0002] The general name of 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid is Febuxostat, which is mainly used for the treatment of hyperuricemia. [0003] [0004] Febuxostat [0005] EP 513379 reports the synthesis method of febuxostat, in which it is mentioned that recrystallization with ethanol is used to obtain the final product, but the problem of the crystal form is not described. In Chinese patent CN1275126, it is recorded that febuxostat has five crystal forms A, B, C, D, G and an amorphous form, wherein crystal A is the relatively stable crystal form, crystal D is methanolate, and crystal G The crystals are hydrates. This patent uses a solvent system of methanol / water or isopropanol / water for crystallization, and can ...

Claims

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Application Information

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IPC IPC(8): C07D277/56A61K31/426A61P19/06
Inventor 隋强王小妹王哲烽时惠麟王小梅孙玮鸿包泳初
Owner SHANGHAI INST OF PHARMA IND
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