An epsilon-caprolactam compound containing a guanidino group structural unit and a preparation method and application thereof

By reacting 1,8-diazabicyclo[5.4.0]undec-7-ene with carbodiimide compounds in a specific solvent, the problem of synthesizing ε-caprolactam compounds containing guanidine structural units was solved, realizing an efficient and economical synthetic method. The product has antimalarial activity and is suitable for drug development.

CN120987848BActive Publication Date: 2026-07-21GUANGZHOU UNIVERSITY
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
GUANGZHOU UNIVERSITY
Filing Date
2025-07-10
Publication Date
2026-07-21

AI Technical Summary

Technical Problem

Existing technologies make it difficult to efficiently synthesize ε-caprolactam compounds containing guanidine structural units, and the methods for synthesizing these compounds are complex and costly, which is difficult to meet the needs of drug development.

Method used

By reacting 1,8-diazabicyclo[5.4.0]undec-7-ene with carbodiimide compounds in a specific solvent, and controlling the temperature and time, a variety of ε-caprolactam compounds containing guanidine structural units were synthesized. The reaction conditions were mild, the raw materials were readily available, and the yield was high.

Benefits of technology

A variety of ε-caprolactam compounds containing guanidine structural units were synthesized efficiently and economically, exhibiting good antimalarial activity and suitable as novel drug intermediates, with a yield of over 56%.

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Abstract

The application belongs to the field of compound synthesis, discloses a epsilon-caprolactam compound containing a guanidyl structural unit and preparation and application thereof, the chemical structure is shown in the following, the epsilon-caprolactam compound containing the guanidyl structural unit has good anti-malaria activity, and is expected to become a new type of pharmaceutical intermediate for preparing anti-malaria drugs.The application also discloses a preparation method of the epsilon-caprolactam compound containing the guanidyl structural unit.The preparation method of the epsilon-caprolactam compound containing the guanidyl structural unit has the advantages that raw materials and catalysts are cheap and easy to obtain, reaction conditions are mild, operation is simple and convenient, the universality of substrates is wide, and a series of epsilon-caprolactam products containing the guanidyl structural unit can all obtain high yield.
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