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Azilsartan polymorphic substance and preparation method thereof

A polymorphic, methanol technology, applied in the field of medicine, can solve the problems of no disclosure of the compound of formula I, no specific disclosure of the compound, etc., and achieve the effects of high yield, easy industrial application, and simple preparation method

Active Publication Date: 2012-11-07
JIANGSU SIMCERE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Neither the priority patent JP1991157194 nor the Chinese patent CN92105152C discloses that the compound of formula I is in crystalline form; in addition, these patents do not specifically disclose whether the compound exists in other solvated forms

Method used

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  • Azilsartan polymorphic substance and preparation method thereof
  • Azilsartan polymorphic substance and preparation method thereof
  • Azilsartan polymorphic substance and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1: the preparation of polymorph A

[0047] Weigh 28.1g of azilsartan into a reaction bottle, add 650mL of anhydrous methanol, heat to reflux, slowly cool down to room temperature after the solid is completely dissolved, filter and recover the precipitated solid, and vacuum dry to constant weight below 40°C. Azilsartan polymorph A was obtained.

Embodiment 2

[0048] Example 2: Preparation of Polymorph A

[0049] Weigh 10g of azilsartan into a reaction bottle, add 150mL of anhydrous methanol and 50mL of water, heat to reflux, cool down to room temperature after all the solids are dissolved, filter and recover the precipitated solid, and vacuum-dry to constant weight below 40°C. Azilsartan polymorph A was obtained.

Embodiment 3

[0050] Example 3: Preparation of Polymorph A

[0051] Weigh 5.2g of azilsartan into a reaction bottle, add 50mL of anhydrous methanol and 100mL of water, heat to reflux, and slowly cool down to room temperature after all the solids are dissolved, filter and recover the precipitated solid, and vacuum dry below 40°C to Constant weight, polymorph A of azilsartan was obtained.

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Abstract

The invention provides an azilsartan polymorphic substance and a preparation method thereof. The azilsartan polymorphic substance is easy to separate and high in stability, has no hygroscopicity, and is an anhydrous polymorphic substance. The preparation method is simple, convenient and easy in industrial application.

Description

technical field [0001] The present invention relates to 2-ethoxy-1-[[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl Polymorphs of ]methyl]-1H-benzimidazole-7-carboxylic acid (azilsartan), and processes for preparing such polymorphs, belong to the field of medicine. Background technique [0002] Azilsartan, namely 2-ethoxy-1-[[2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)biphenyl- 4-yl]methyl]-1H-benzimidazole-7-carboxylic acid, the structure of which is shown in Formula I. The drug is a selective angiotensin II receptor antagonist (ARB for short) developed by Takeda Corporation of Japan. It has antihypertensive and central nervous effects and can be used alone or together with other antihypertensive drugs. In January 2012, the Japanese Ministry of Health and Welfare approved the listing in Japan for the treatment of hypertension. [0003] [0004] The subject of Example 1 of Chinese patent CN92105152C (priority patent JP1991157194) discloses the preparation met...

Claims

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Application Information

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IPC IPC(8): C07D413/10
Inventor 陈琪朱玉成张连第丁磊
Owner JIANGSU SIMCERE PHARMA
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