A process for the preparation of imidazolone derivatives

By using rare-earth Lewis acids to catalyze the reaction of isocyanates and polysubstituted propargylamines, the problems of complex synthesis and low yield of existing imidazolide compounds have been solved, realizing the efficient and simple preparation of imidazolide derivatives, which are suitable for the synthesis of various drug molecule fragments.

CN122355944APending Publication Date: 2026-07-10QUZHOU CITY PEOPLE HOSPITAL +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
QUZHOU CITY PEOPLE HOSPITAL
Filing Date
2026-06-05
Publication Date
2026-07-10

AI Technical Summary

Technical Problem

Existing methods for synthesizing imidazolide compounds are cumbersome and have low yields, making them unsuitable for large-scale industrial production. Furthermore, existing catalytic systems suffer from poor feedstock selectivity and numerous byproducts.

Method used

Using isocyanate and polysubstituted propargylamine as raw materials, the reaction is carried out under the catalysis of rare earth Lewis acid to form imidazolidinone derivatives. The rare earth trifluoromethanesulfonic acid complex is preferred as the catalyst. Organic solvents such as toluene are used, and the reaction time and temperature are controlled to achieve one-step efficient construction of CN single bonds and new imidazolidinone rings.

Benefits of technology

The reaction is mild, the operation is simple, the product yield is high, the raw materials are readily available, it has good functional group compatibility, a wide range of applications, and improves the synthesis efficiency and atom economy.

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Abstract

This invention discloses a method for preparing imidazolidinone derivatives, belonging to the field of pharmaceutical synthesis technology. The method involves reacting isocyanate and polysubstituted propargylamine as raw materials in an organic solvent under rare-earth Lewis acid catalysis to obtain the target imidazolidinone derivative. This invention features a mild reaction, simple operation, improved atom economy and synthetic efficiency, and good functional group compatibility.
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Citation Information

Patent Citations

  • A 2-imidazolone derivative and its application

    CN116354924B