Synthetic technology of azelastine hydrochloride

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 ...