A method for microwave-accelerated synthesis of loxoprofen

By using cyclopentanone as a starting material and microwave-promoted enamine alkylation reaction, the problems of equipment corrosion, high impurity content, and low yield in the synthesis of loxoprofen sodium were solved, achieving low-cost and high-efficiency production of loxoprofen sodium.

CN122233865APending Publication Date: 2026-06-19XIAMEN MEDICAL COLLEGE
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
XIAMEN MEDICAL COLLEGE
Filing Date
2026-01-29
Publication Date
2026-06-19

AI Technical Summary

Technical Problem

The existing synthesis route for loxoprofen sodium suffers from problems such as high-temperature corrosion of equipment, generation of large amounts of wastewater and waste acid, carbonization of products, high impurities, and unsatisfactory purity. Furthermore, the enamine alkylation reaction has a long reaction time and low yield, resulting in high production costs and low efficiency.

Method used

Using cyclopentanone as the starting material, the enamine alkylation reaction is promoted by microwave, combined with a mild hydrolysis decarboxylation process, avoiding the use of highly corrosive hydrobromic acid, shortening the reaction time to 10-20 minutes, and improving the yield.

Benefits of technology

This method enables low-cost and efficient synthesis of loxoprofen sodium, avoiding equipment corrosion and carbonization, simplifying purification steps, and improving product purity and yield.

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Abstract

This invention discloses a microwave-promoted synthesis method for loxoprofen. The method involves reacting cyclopentanone and tetrahydropyrrole with a dehydrating agent to generate 1-(1-pyrrolidine)cyclopentene, which is then reacted with 2-(4-halomethylphenyl)propionate under microwave heating to undergo an enamine alkylation reaction. The resulting product is hydrolyzed with hydrochloric acid to generate 2-(4-((2-oxocyclopentyl)methyl)phenyl)propionate, which is then hydrolyzed in NaOH solution and acidified with hydrochloric acid to obtain loxoprofen. This method uses cyclopentanone as a starting material instead of the expensive 2-ethoxycarbonylcyclopentanone, which is readily available and low-cost. The microwave-promoted enamine alkylation reaction results in a short reaction time, high efficiency, and high yield. Furthermore, it avoids the use of highly corrosive hydrobromic acid for hydrolysis and decarboxylation, making it more environmentally friendly.
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