Synthesis method for montelukast

• Main Authors: ZHANG ZHAOZHEN, YANG QINGKUN, JIANG HAIPING, WU KE, ZHOU XUEWEN, ZHOU XIANGUO, GAO DALONG, YANG BOYONG, DONG TINGHUA
• Format: Patent
• Language: Chinese; English
• Published: 04.05.2016
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention discloses a synthesis method for montelukast. 1-(mercaptomethyl)- cyclopropaneacetic acid and alkali are added into organic solvent, and the mixture is subjected to a stirred reaction at 10 DEG C-30 DEG C to obtain a dianion alkaline solution; a quinolinediol compound and triethylamine are dissolved into organic solvent to obtain a quinolinediol solution; paratoluensulfonyl chloride is dissolved into organic solvent to obtain a paratoluensulfonyl chloride solution; then flow speed is controlled to inject the quinolinediol solution and the paratoluensulfonyl chloride into a micro-reactor for a mixed reaction at 10 DEG C-30 DEG C to obtain a tosylate compound solution; then the tosylate compound solution and the injected 1-(mercaptomethyl)-cyclopropaneacetic acid dianion alkaline solution are subjected to a mixed reaction at 10 DEG C-30 DEG C to obtain montelukast feed liquid which is discharged out of the micro-reactor, and the montelukast solid is obtained through post-treatment. The synthesis m