Preparation method of aryl propionic acid non-steroidal anti-inflammatory drugs
By using two-step reactions of arylethylene and cyanotylation reagent under the action of nickel catalyst, the intermediate α-substituted phenyl propionitrile was generated and hydrolyzed, and the problems of low reaction yield and high preparation cost in the prior art were solved, and efficient and low-cost preparation of aryl propionic acid drugs were achieved.
CN119751233APending Publication Date: 2025-04-04ZHEJIANG PHARMA COLLEGE
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Patent Information
- Application Number
- CN202411951993.0
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2024-12-27
- Publication Date
- 2025-04-04
AI Technical Summary
Technical Problem
The existing preparation methods for aryl propionic acid drugs have problems such as low reaction yield, high preparation cost and strict operating conditions.
Method used
Using arylethylene and cyanotylation reagent as raw materials, under the action of nickel catalyst and ligand, the intermediate α-substituted phenylpropionitrile was formed through two-step reaction, and then hydrolyzed under acidic conditions to obtain the target product.
Benefits of technology
Aromatic ring α-position cyanolysis is achieved, β-position cyanolysis by-products are reduced, reaction yield and product quality are improved, preparation costs are reduced, and it is suitable for industrial production.
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Abstract
The present invention relates to the technical field of drug synthesis, and in particular to a method for preparing an aryl propionic acid non-steroidal anti-inflammatory drug, comprising the following steps: in an organic solvent, using arylethylene and a cyanation reagent as raw materials, generating α-substituted phenyl propionitrile through a cyanation reaction under the action of a nickel catalyst and a ligand; hydrolyzing the α-substituted phenyl propionitrile under acidic conditions to obtain an aryl propionic acid non-steroidal anti-inflammatory drug, the present invention explores the introduction of an isopropyl cyano group on an aromatic group under the catalysis of a cheap nickel catalyst, and then hydrolyzing to generate an aryl propionic acid non-steroidal anti-inflammatory drug preparation method, and the synthesis process has great industrial feasibility. The preparation method of the present invention is in line with the development direction of green and environmentally friendly drug synthesis, has a high yield, mild reaction conditions, is suitable for industrialization, and can achieve greater scientific value and social benefits.
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