Preparation method of montelukast

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 comp...

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Main Authors ZHANG ZHAOZHEN, YANG QINGKUN, JIANG HAIPING, WU KE, ZHOU XUEWEN, ZHOU XIANGUO, GAO DALONG, YANG BOYONG, DONG TINGHUA
Format Patent
LanguageChinese
English
Published 04.05.2016
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary: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.
Bibliography:Application Number: CN201610097120