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Montelukast di-n-propylamine salt crystal form and preparation method and application

A technology of n-propylamine salt and di-n-propylamine, which is applied in the crystal form of montelukast di-n-propylamine salt and its preparation and application fields, can solve the problems of low impurity removal efficiency and complicated operation, and achieve high purity, simple preparation, and high yield. high rate effect

Active Publication Date: 2015-10-28
ZHEJIANG CHARIOTEER 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, the operation is too complicated and the removal efficiency is very low

Method used

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  • Montelukast di-n-propylamine salt crystal form and preparation method and application
  • Montelukast di-n-propylamine salt crystal form and preparation method and application
  • Montelukast di-n-propylamine salt crystal form and preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Add 20g (0.034 moles) of montelukast acid to 500ml of acetone, replace with nitrogen twice, add 6.97ml (0.051 moles) of di-n-propylamine, stir until the material solution is clear, add seed crystals, stir at 0°C for 16h, filter, After drying, 21.4 g of montelukast di-n-propylamine salt crystal form was obtained, with a content of 99.6% and a yield of 91.3%.

[0027] Infrared spectrum, DSC spectrum, XRD spectrum of montelukast di-n-propylamine salt crystal form, such as figure 1 , figure 2 and image 3

Embodiment 2

[0029] Add 20g (0.034 moles) of montelukast acid to 200ml of toluene, stir evenly, replace with nitrogen twice, add 5.11ml (0.0374 moles) of di-n-propylamine, stir until the material solution is clear, add seed crystals, and stir at 25°C for 24h . Filter and dry. 21.5 g of montelukast di-n-propylamine salt crystalline form with less than 0.1% impurity was obtained, with a content of 99.8% and a yield of 91.7%.

Embodiment 3

[0031] Add 20g (0.034 moles) of montelukast acid to 100ml of toluene, stir evenly, replace with nitrogen twice, add 4.65ml (0.034 moles) of di-n-propylamine, stir until the material liquid is dissolved, and stir at 30°C for 32h. Filter and dry. 19.5 g of montelukast di-n-propylamine salt crystalline form with less than 0.1% impurity was obtained, with a content of 99.6% and a yield of 83.2%.

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Abstract

The invention discloses a Montelukast di(n-propyl) amine salt crystal form and a preparation method and application thereof. By Cu-K alpha radiation, the crystal form has characteristic absorption peaks at the positions of 2theta in degrees of 7.55 plus or minus 0.2, 8.71 plus or minus 0.2, 9.88 plus or minus 0.2, 11.84 plus or minus 0.2, 15.10 plus or minus 0.2, 15.88 plus or minus 0.2, 17.21 plus or minus 0.2, 18.56 plus or minus 0.2, 19.73 plus or minus 0.2, 20.90 plus or minus 0.2, 21.84 plus or minus 0.2, 22.60 plus or minus 0.2, 23.52 plus or minus 0.2, 25.18 plus or minus 0.2, 26.44 plus or minus 0.2, 27.98 plus or minus 0.2, 28.86 plus or minus 0.2 and 29.62 plus or minus 0.2. The preparation method of the Montelukast di(n-propyl) amine salt crystal form comprises the steps of salifying Montelukast acid and di(n-propyl) amine in organic solvent A and dissolving out to obtain the Montelukast di(n-propyl) amine salt crystal form, wherein the organic solvent A is methylbenzene or C3-C5 ketone or methylbenzene and C3-C5 ketone mixed solvent. The crystal form is applied to preparation of high-purity Montelukast sodium.

Description

(1) Technical field [0001] The present invention relates to a crystal form of montelukast di-n-propylamine salt and its preparation method and application (2) Background technology [0002] The chemical name of Montelukast Sodium is: 1-(((1-(R)-(3-(2-(7-chloro-2-quinolinyl)phenyl)-3-(2 -(1-Hydroxy-1-methylethyl)phenyl)thio))methyl)sodium cyclopropylacetate, the structural formula is as follows: [0003] [0004] The compound can be used to treat respiratory diseases such as asthma and allergic rhinitis. Merck's patent US5565473 discloses the chemical structural formula of montelukast sodium and its preparation method, wherein the montelukast acid obtained by the reaction is an oil, and after column chromatography purification, the sodium salt is dissolved in water and freeze-dried , because the intermediate and the final product all need column purification and the yield is low, so this preparation method is not suitable for large-scale production. Existing patents and...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D215/18C07C211/06C07C209/00
CPCC07D215/18
Inventor 蒲通张飞飞范一陈恬王乃星杨建明
Owner ZHEJIANG CHARIOTEER PHARMA
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