Preparation process of montelukast sodium and its intermediate product

A technology of montelukast sodium and preparation process, applied in the field of drug synthesis, can solve the problems of high price of montelukast sodium, increased production cost, increased medical cost of patients, etc., and achieves simple operation, high total yield, The effect of low production cost
CN104293850BActive Publication Date: 2017-08-04JIANGSU HANSYN PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
JIANGSU HANSYN PHARMA
Publication Date
2017-08-04

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Abstract

The present invention discloses a montelukast sodium preparation technology and intermediates; 7-chloro-2-methylquinine and 3-bromobenzaldehyde are used as raw materials for condensation reaction to obtain a compound A2; by carbon-carbon coupling of the compound A2 and 1-tetralone in the presence of a catalyst, an intermediate compound A3 is obtained; an important intermediate compound A4 is obtained by bio-enzyme catalyzed asymmetric Baeyer-villiger reaction, a chiral center is highly selectively constructed, an important intermediate compound A5 is prepared from the compound A4 by grignard reaction by use of methylmagnesium chloride, finally montelukast sodium (A6) is obtained; according to the technology, the highly chiral important intermediate compound A4 is obtained by bio-enzyme catalyzed asymmetric reaction, the catalyst can be effectively repeatedly used, and the kind of used solvents is less, and the montelukast sodium preparation technology has the characteristics of safety and environmental protection, greatly saves the production cycle, is low in production cost, high in total yield, and simple in operation of production units, and is suitable for industrialized production.
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Description

technical field

[0001] The invention relates to a preparation process of montelukast sodium and an intermediate product thereof, belonging to the technical field of medicine synthesis. Background technique

[0002] The chemical name of Montelukast Sodium is: 1-(((1-(R)-(3-(2-(7-chloro-2-quinolinyl)-vinyl)phenyl)- Sodium 3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio))methyl)cyclopropylacetate, the structural formula is as follows:

[0003]

[0004] Montelukast is currently the only strong selective leukotriene receptor antagonist that is taken once a day, and is suitable for the treatment of asthma and allergic rhinitis asthma syndrome in adults and children. The compound first disclosed the chemical structure and preparation method of montelukast in US5565473 by Merck, and reported the preparation method of the compound in detail in process patents CN1046712 and CN1139429. Due to its wide application range and convenient administration, it is currently It has been wi...

Claims

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