Preparation method of pranlukast intermediate

A technology of intermediates and schemes, applied in the field of preparation of Prenstedt intermediates, can solve the problems of severe reaction conditions, difficulty in tetrazole, difficult removal of impurities, etc., and achieve high purity, great potential for economic value, and convenient operation Effect

Pending Publication Date: 2021-11-26
HUNAN FURUI BIOPHARMA TECH CO LTD
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  • Abstract
  • Description
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  • Application Information

AI Technical Summary

Problems solved by technology

[0012] ④Giles, Hideki, and Hayler all add substituents to tetrazole to make the condensation reaction easier, but it is difficult to synthesize tetrazole with substituents on nitrogen, and the final removal reaction uses dangerous lithium aluminum tetrahydrogen, etc. Reagent, not easy to industrialize
[0014] The above routes generally have the disadvantages of severe reaction conditions, low yield, high toxicity and difficult removal of impurities produced by the reaction.

Method used

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  • Preparation method of pranlukast intermediate
  • Preparation method of pranlukast intermediate
  • Preparation method of pranlukast intermediate

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Embodiment Construction

[0029] The technical solutions of the present invention will be clearly and completely described below in conjunction with the embodiments of the present invention. Apparently, the described embodiments are only some of the embodiments of the present invention, not all of them. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without creative efforts fall within the protection scope of the present invention.

[0030] A kind of preparation method of Pronstedt intermediate, comprises the steps:

[0031] Q1. React with compound C as a raw material, and finally obtain compound D. The characteristics of compound D are: R1 is a halogen, a group that can be polymerized with a hydroxyl group to form an ether; the position of R2 is an ester group;

[0032] Q2. After compound D is condensed with o-acetaminophenol, compound B is prepared through ring-forming reaction and hydrolysis reaction, and finally prepared wit...

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Abstract

The invention provides a preparation method of a pranlukast intermediate. A compound C serving as a raw material reacts obtain the pranlukast intermediate. The preparation method has the advantages that the reaction condition is relatively mild, the operation is convenient, the purity and the yield of the obtained pranlukast intermediate are high, and the method is suitable for industrial production, so that a more valuable synthesis route is provided for preparation of pranlukast, good social benefits and economic benefits can be generated, and the economic potential is great.

Description

technical field [0001] The present invention relates to the technical field of organic synthesis and pharmacy, and more specifically, relates to a preparation method of a Prensted intermediate used for making Prensted medicine. Background technique [0002] Prenzact is a new type of anti-asthma drug listed in the mid-nineties, and it is one of the three leukotriene receptor antagonists widely concerned in the world at present. Prenzact is characterized by extremely low toxicity (oral LD50 greater than 2000mg / kg), for 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. [0003] The structural characteristics of Pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/04
CPCC07D405/04
Inventor 鲁光英
Owner HUNAN FURUI BIOPHARMA TECH CO LTD
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