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Preparation method of montelukast sodium

A technology of montelukast sodium and montelukast acid, which is applied in the field of chemical pharmaceuticals, can solve the problems of complex operation and low efficiency of impurity removal, and achieve the effect of reducing the content of impurities

Active Publication Date: 2016-09-07
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method involves a large amount of extraction and washing solvents, the operation is complicated and the removal efficiency is very low
[0009] As the market has higher and higher quality requirements for raw materials (API), simply meeting the pharmacopoeia standards is not enough to meet the requirements, and there is an urgent need to develop a method suitable for industrial production of high-quality montelukast sodium salt

Method used

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  • Preparation method of montelukast sodium
  • Preparation method of montelukast sodium
  • Preparation method of montelukast sodium

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1: a kind of preparation method of montelukast sodium, specifically as follows:

[0035] A. Add 50g of crude montelukast acid, 250mL of ethyl acetate, and 9.96mL of 2-amino-1-butanol to a 500mL three-necked flask in sequence, stir to dissolve, control the temperature at 15-25°C and stir for 5 hours, suction filter, 50 After vacuum drying at ℃ for 6 hours, montelukast acid 2-amino-1-butoxide was obtained with a yield of 92%.

[0036] B. Add 50g of montelukast acid 2-amino-1-butoxide and 400mL of toluene to a 1000mL three-necked flask in turn, reflux until dissolved, lower the temperature, control the temperature at 5-10°C, crystallize for 5 hours, and filter with suction. Vacuum drying at 60° C. for 8 hours gave montelukast acid 2-amino-1-butoxide with a yield of 95%.

[0037] C. Add 50g of montelukast acid 2-amino-1-butoxide and 400mL of dichloromethane to a 1000mL three-necked flask successively, and add aqueous acetic acid solution (10mL of acetic acid, di...

Embodiment 2

[0039] Embodiment 2: a kind of preparation method of montelukast sodium, specifically as follows:

[0040] A. Add 50g of crude montelukast acid, 350mL of ethyl acetate, and 8.3mL of 2-amino-1-butanol to a 500mL three-neck flask in sequence, stir to dissolve, control the temperature at 15-25°C for 4 hours, and suction filter, 50 °C and vacuum dried for 6 hours to obtain montelukast acid 2-amino-1-butoxide with a yield of 90%.

[0041] B. Add 50g of montelukast acid 2-amino-1-butoxide and 700mL of toluene to a 1000mL three-necked flask in turn, reflux until dissolved, lower the temperature, control the temperature at 20-25°C, crystallize for 5 hours, and filter with suction. After vacuum drying at 60°C for 8 hours, montelukast acid 2-amino-1-butoxide was obtained with a yield of 92.5%.

[0042] C. Add 50g of montelukast acid 2-amino-1-butoxide and 500mL of dichloromethane to a 1000mL three-necked flask successively, and add aqueous acetic acid solution (10mL of acetic acid, dil...

Embodiment 3

[0044] Embodiment 3: a kind of preparation method of montelukast sodium, specifically as follows:

[0045] A. Add 50g of crude montelukast acid, 500mL of ethyl acetate, and 20.74mL of 2-amino-1-butanol to a 500mL three-necked flask in sequence, stir to dissolve, control the temperature at 15-25°C and stir for 5 hours, then suction filter, 50 After vacuum drying at °C for 6 hours, montelukast acid 2-amino-1-butoxide was obtained with a yield of 86.6%.

[0046] B. Add 50g of montelukast acid 2-amino-1-butoxide and 400mL of toluene to a 1000mL three-necked flask in sequence, reflux until dissolved, lower the temperature, control the temperature at 20-30°C, crystallize for 20 hours, and filter with suction. After vacuum drying at 60°C for 8 hours, montelukast acid 2-amino-1-butoxide was obtained with a yield of 92.1%.

[0047] C. Add 50g of montelukast acid 2-amino-1-butoxide and 600mL of dichloromethane to a 1000mL three-necked flask successively, and add aqueous acetic acid sol...

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Abstract

The invention discloses a preparation method of montelukast sodium. The method comprises: A, converting a montelukast acid crude into a montelukast amino acid 2-amino-1-butanol salt; B, recrystallizing and refining the montelukast amino acid 2-amino-1-butanol salt; C, acidizing the montelukast amino acid 2-amino-1-butanol salt after refining, and freeing to obtain high-purity montelukast acid; and D, converting the montelukast acid into montelukast sodium. The preparation method of montelukast sodium has the advantages of simple process, high yield and good impurity removing effect, and the purity of the prepared montelukast sodium is more than 99.9%.

Description

technical field [0001] The invention belongs to the technical field of chemical pharmacy, and in particular relates to a preparation method of montelukast sodium. Background technique [0002] The chemical name of montelukast sodium is 1-(((1-(R)-(3-(2-(7-chloro-2-quinolyl)-vinyl)phenyl)-3-(2-hydroxy -1-tolyl ethyl) phenyl) propyl) thio)) methyl) sodium cyclopropyl acetate, its structural formula is as follows: [0003] [0004] Montelukast Sodium is a new type of highly selective LTD developed by Merck & Co. 4 Receptor antagonist, this drug acts as Selective Leukotriene LTD 4 Receptor antagonist, can interact with leukotrienes LTD in the airway 4 Selective combination of receptors blocks the action of allergic mediators, improves respiratory inflammation, and makes airways unobstructed. It is an anti-inflammatory and anti-allergic drug with high efficiency, low toxicity and good safety. In recent years, with the gradual expansion of the application market of monteluk...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D215/18
CPCC07D215/18
Inventor 张贵民冯启国徐新福
Owner SHANDONG NEWTIME PHARMA
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