Preparation method of 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 preparation method of montelukast. An inorganic base solution is cooled to 0-10 DEG C, 1-(mercaptomethyl)-cyclopropaneacetic acid is added, and a stirred reaction is performed to obtain a 1-(mercaptomethyl)-cyclopropaneacetic acid dianion base solution; a quinolinediol compound is dissolved into water, and inorganic base and a phase transfer catalyst are added for stirring and even mixing; after the mixture is cooled to 0-10 DEG C, paratoluensulfonyl chloride is added for a reaction to obtain a tosylate compound solution, and then the tosylate compound solution is added into the 1-(mercaptomethyl)-cyclopropaneacetic acid dianion base solution for a stirred reaction to obtain a water solution of montelukast; then the montelukast solid is obtained through post-treatment. The method is simple in technology, mild in reaction condition, economical, environmentally friendly and high in yield and makes industrialized production easy.