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Purification method of olmesartan

A technology for olmesartan medoxomil and a purification method, which is applied in the field of purification of high-purity bulk drug products, can solve the problems of easy excess of residual solvent in the product, difficult to produce by industrialized methods, slow crystallization speed, etc., and achieves low degradation risk and drying. The effect of short time and fast crystallization speed

Inactive Publication Date: 2015-12-09
JIANGSU ZHONGBANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The present invention solves the disadvantages of slow crystallization speed of the product in the above method, difficulty in drying due to water as a poor solvent, easy excess of residual solvent in the product, and difficulty in industrialized production.

Method used

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  • Purification method of olmesartan
  • Purification method of olmesartan

Examples

Experimental program
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Effect test

Embodiment 1

[0023] Put 10 g of crude olmesartan medoxomil and 80 g of methanol into the reaction flask, heat under reflux and stir to dissolve. After dissolution is completed, the solution is cooled to 40±5°C. After cooling down, add 160g petroleum ether dropwise to the bottle. After the dropwise addition is completed, the temperature in the bottle is reduced to 10°C, stirred for 2 hours to crystallize, filtered, and vacuum dried to obtain olmesartan medoxomil 8.5kg, yield 85.0%, HPLC purity 99.93 %.

Embodiment 2

[0025] Put 10g olmesartan medoxomil and 100g acetone into the reaction flask, heat under reflux and stir to dissolve. After the dissolution is completed, the solution is cooled to 30±5°C. After cooling, add 100g of isopropyl ether dropwise to the bottle. After the dropping, the temperature in the bottle is reduced to -10°C, stirred for 2 hours to crystallize, filtered and dried in vacuum to obtain 8.9g of Olmesartan medoxomil with a yield of 89.0%. HPLC The purity is 99.89%.

Embodiment 3

[0027] Put 10g of crude olmesartan medoxomil and 100g of acetonitrile into the reaction flask, heat to reflux and stir to dissolve, after dissolving, cool the solution to 30±5°C. After cooling down, add 200g methyl tert-butyl ether dropwise to the bottle. After the dropwise addition is complete, reduce the temperature in the bottle to 0°C, stir and crystallize for 2 hours, filter, and vacuum dry to obtain olmesartan medoxomil with a yield of 92.0%. , HPLC purity 99.90%.

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PUM

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Abstract

The invention provides a purification method of olmesartan, and particularly relates to a novel purification method of olmesartan. The purification method comprises the steps of: enabling the olmesartan to be dissolved in ethanol, acetone or acetonitrile, and dropwise adding an ether type poor solvent for cooling and crystallization so as to obtain highly-purified olmesartan. The purification method disclosed by the invention has advantages that the operation is simple, products are easy to be separated and dried, and the yield is high and the like.

Description

Technical field [0001] The present invention relates to a purification technology of high-purity bulk drug products, and more specifically relates to a purification method of olmesartan medoxomil. technical background [0002] The chemical name of Olmesartan medoxomil is 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[[2'-(1H-tetrazol-5-yl)[1,1' -Biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic acid (5-methyl-2-oxy-1,3-dioxol-4-yl)methyl Esters (MerckIndex, 13th edition). [0003] The chemical structure of Olmesartan medoxomil is as follows: [0004] [0005] Olmesartan medoxomil is a drug premise. It is an orally effective non-peptide angiotensin II receptor antagonist developed by Japan's Daiichi Sankyo Company. The drug was approved by the U.S. FDA in May 2002, with the trade name Banicar and the specifications of 5mg, 20mg and 40mg. It was approved in Germany in August of the same year and was listed under the trade name Olmetec in early October. Its outstanding advantage is that it...

Claims

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Application Information

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IPC IPC(8): C07D405/14
CPCC07D405/14
Inventor 杨柳钱刚朱正航韩小军赵华阳
Owner JIANGSU ZHONGBANG PHARMA
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