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Synthesis technology of intermediate of anti-asthma drug namely pranlukast

A synthesis process and intermediate technology, which is applied in the field of synthesis process of the anti-asthma drug Prenster intermediate, which can solve the problems of low yield, high cost, and high toxicity, and achieve high yield, low cost, and convenient operation Effect

Inactive Publication Date: 2015-03-11
PINGHU UCON PHARMA R&D
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Problems solved by technology

There have been some reports on the synthesis process of Prenstedt intermediates, but they all generally have the disadvantages of high cost, low yield and high toxicity

Method used

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  • Synthesis technology of intermediate of anti-asthma drug namely pranlukast

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Embodiment Construction

[0017] The present invention will be further described below in conjunction with specific examples.

[0018] The synthetic process step of the present invention is as follows:

[0019] Step (1) etherification reaction:

[0020] Mix the raw material 4-hydroxybenzoic acid methyl ester with a base and a solvent to obtain a raw material mixture, then add 4-phenylbromobutane to the raw material mixture, and then heat for reaction. The 4-phenylbromobutane: 4- Methyl hydroxybenzoate: the molar ratio of alkali is 1:1.0~1.1:1.3~1.5; the reaction solution after heating and reacting is poured into ice water to obtain 4-(4-phenylbutoxy)methyl benzoate, the The weight ratio of ice water:solvent is 6~8:1.

[0021] Step (2) hydrolysis reaction:

[0022] Mix the 4-(4-phenylbutoxy)methyl benzoate obtained in step (1) with sodium hydroxide solution and a solvent, and then heat for reaction. The sodium hydroxide and 4-(4-phenylbutoxy Base) The molar ratio of methyl benzoate ...

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Abstract

The invention relates to a synthesis technology of an intermediate [4-(4-phenylbutoxy)benzoic acid] of an anti-asthma drug namely pranlukast. The synthesis technology comprises the following steps: (1) carrying out etherification reactions; (2) performing hydrolysis reactions. The 4-(4-phenylbutoxy)benzoic acid is prepared through esterification and hydrolysis, the synthesis route has the characteristics of low cost, mild reaction conditions, low toxicity, convenient operation, high yield, and suitability for the industrial production.

Description

technical field [0001] The invention relates to a synthesis process of an anti-asthma drug Prenstedt intermediate, belonging to the field of drug synthesis. Background technique [0002] Prensted intermediate, its chemical name is 4-(4-phenylbutoxy)benzoic acid, its structural formula is: [0003] [0004] Prenast is a new type of anti-asthma drug listed in the mid-1990s, and it is one of the three leukotriene receptor antagonists that are widely concerned in the world. Prenster is characterized by very low toxicity (oral LD 50 greater than 2000mg / kg). to LTC 4 、LTD 4 , LTE 4 significantly inhibited, especially for LTD 4 (the main component that causes the contraction of human tracheal smooth muscle) has a significant inhibitory effect, and is clinically effective not only for atopic asthma, but also for infectious, mixed, chronic, paroxysmal and non-seasonal bronchial asthma; Severe adverse reactions, no effect on p450 drug enzymes, no drug interaction problems. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C65/24C07C51/02
CPCC07C67/30C07C51/09C07C69/92C07C65/24
Inventor 忻华钟全发史黎辉
Owner PINGHU UCON PHARMA R&D
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