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Synthetic technology of azelastine hydrochloride

A technology of azelastine hydrochloride and synthesis process, which is applied in directions such as organic chemistry, can solve the problems of low yield and difficulty in obtaining raw materials, and achieves the effects of high yield and simple process

Inactive Publication Date: 2012-03-28
GUIZHOU YUNFENG PHARMA
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  • Abstract
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Problems solved by technology

[0004] In 2009, Chinese patent CN20091014407.0 used N-methylhexahydroazepin-4-one hydrochloride as raw material, and synthesized azepine hydrochloride by condensation in one step Ting, the total yield reached 67%, but the raw materials used in this method are difficult to obtain, and the yield is not high

Method used

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Embodiment Construction

[0014] A kind of synthetic technique of azelastine hydrochloride of the present invention, adopts N-methylhexahydroazepin-4-one hydrochloride and benzohydrazine to form hydrazone, then reduces with potassium borohydride, finally and Condensation of 2-(p-chlorophenylacetyl)benzoic acid to 4-(4-chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepine-4-yl)-1-(2H)- Phthalazine hydrochloride.

[0015] Add 100 mol of N-methylhexahydroazepine-4-one hydrochloride and 110 mol of benzohydrazide to the reaction kettle, stir and react at room temperature for 1-5h, then cool to 0 with ice-salt water or ice-salt bath ~20°C; add 50L of methanol solution of 2 mol / L KOH dropwise for 5h, then add 130mol of potassium borohydride, continue cooling and stirring for 30 minutes, then stir and react at 40~50°C for 6h; 2 Cl 2（ Extraction (1000ml×3), with 50kg MgSO 4 After drying, add ether solution containing HCl to form a salt and desolventize; then add 1000kg of pure water and 100mol of 2-(p-chlorophen...

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Abstract

The invention discloses a synthetic technology of azelastine hydrochloride, which is characterized in that acylhydrazone is formed by N-Methylhexahydroazepin-4-one hydrochloride and benzoyl hydrazine and then is reduced with potassium borohydride, and finally is condensed with 2-(para chlorobenzene acetyl) benzoic acid into 4-( chlorine benzyl)-2-piperazidine-1- methyl-1H-azelastine-4- radical)-1-(2H)-phthalazine hydrochloride. The synthetic technology has the advantages of simple process and higher yield.

Description

technical field [0001] The invention belongs to the field of fine chemical production, and in particular relates to a synthesis process of azelastine hydrochloride. Background technique [0002] The chemical formula of azelastine hydrochloride is 4-(4-chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepine-4-yl)-1-(2H)-phthalazine hydrochloride , was developed by Asta-Werker AG of Germany and Eisai of Japan, and has received extensive attention since its listing. At present, the product is produced in the United States, Germany, Britain, Japan and France, and has been included in the British Pharmacopoeia. It is expected that the launch of the new anti-asthma drug azelastine hydrochloride will greatly change the current drug structure for the treatment of allergic rhinitis and asthma. It has huge market space and prospects, and the research on its technology is of great significance. [0003] Chinese Journal of Pharmaceutical Industry reported in 2003 that N-methylpiperidin-4-one ...

Claims

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Application Information

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IPC IPC(8): C07D403/04
Inventor 陈友黄忠文刘诚李占胜倪全平
Owner GUIZHOU YUNFENG PHARMA
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