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2-(3-cyano-4-isobuoxy phenyl)4-methyl-5-thiazole aminic acid crystal and preparation method thereof

A technology of isobutoxyphenyl and thiazolecarboxylic acid, applied in the field of 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid crystal form and its preparation, Can solve problems such as the problem of not describing the crystal form

Active Publication Date: 2010-05-12
SHANGHAI INST OF PHARMA IND CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] 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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  • 2-(3-cyano-4-isobuoxy phenyl)4-methyl-5-thiazole aminic acid crystal and preparation method thereof
  • 2-(3-cyano-4-isobuoxy phenyl)4-methyl-5-thiazole aminic acid crystal and preparation method thereof
  • 2-(3-cyano-4-isobuoxy phenyl)4-methyl-5-thiazole aminic acid crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The preparation method of febuxostat crystal form I:

[0027] Add 1.7 g of febuxostat to 30 ml of ethyl acetate to dissolve under reflux, then cool to room temperature while stirring, and filter after 2 hours. Dry at 60°C for 2 hours. 1.5 g of a sample of crystal form I was obtained. The melting point is 208-209°C.

Embodiment 2

[0029] The preparation method of febuxostat crystal form I:

[0030] Add 0.5 g of febuxostat to 5 ml of ethyl acetate and reflux to dissolve, then cool to room temperature under stirring, after 2 hours, filter and dry at 60 ° C for 2 hours to obtain 0.4 g of a sample of crystal form I. The melting point is 208-209 ° C.

Embodiment 3

[0032] The preparation method of febuxostat crystal form I:

[0033] Add 1.0 g of febuxostat to 100 ml of ethyl acetate and heat to dissolve at 20°C, then cool to room temperature while stirring, and filter after 2 hours. Dry at 60°C for 2 hours. A 0.9 g sample of Form I was obtained. The melting point is 208-209°C.

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Abstract

The present invention discloses two crystal models and the preparation method of the anti-hyperuricemia drug 2-(3-ayano-4-isobuoxy phenyl)-4-methyl-5- thiazole acid. The preparation method of the crystal models commonly uses the low-toxicity ethanol, ethyl acetate or acetone as the solvent; the safety is relatively high. In addition, the hygroscopicity of the two crystal models is low in the high-humidity environment and the two crystal models are suitable for the steady pharmaceutical preparation.

Description

technical field [0001] The invention relates to two crystal forms 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] 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 perform crystal transformation according to different drying methods. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D277/56
Inventor 隋强王小妹王哲烽时惠麟
Owner SHANGHAI INST OF PHARMA IND CO LTD
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