A gemfibrozil deuterium derivative, and a preparation method and application thereof

By synthesizing deuterated gemfibrozil derivatives under alkali metal catalysts and deuterium source reagents, the problems of rapid in vivo metabolism and toxic metabolite formation of gemfibrozil have been solved, thereby improving the stability and safety of the drug and making it suitable for the treatment of hyperlipidemia and Alzheimer's disease.

CN120698876BActive Publication Date: 2026-06-09SHANGHAI ESKET TECH CO LTD
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Patent Information

Application Number
CN202510730656.7
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2025-06-03
Publication Date
2026-06-09
Estimated Expiration
2045-06-03

AI Technical Summary

Technical Problem

Existing gemfibrozil drugs are rapidly metabolized in the body, leading to the formation of toxic metabolites and posing a potential carcinogenic risk. There is a lack of synthetic methods for selective deuteration reactions.

Method used

Using gemfibrozil as the starting material, a hydrogen-deuterium exchange reaction was carried out in the presence of an alkali metal catalyst and a deuterium source reagent to synthesize a deuterated derivative of gemfibrozil. This simplified process and improved the yield, making it suitable for industrial production.

Benefits of technology

The deuterated derivatives of gemfibrozil synthesized through a simplified process extend the drug's half-life, reduce the formation of toxic metabolites, and improve drug stability and safety, making them suitable for the treatment of hyperlipidemia and Alzheimer's disease.

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Abstract

The application discloses a gemfibrozil deuterated derivative as shown in formula (I) and a preparation method and application thereof, and belongs to the field of organic and pharmaceutical synthesis. The method has simple preparation process and low cost. The gemfibrozil deuterated derivative synthesized by the method has the advantages of high purity and high deuterium substitution rate. The application also discloses application of the gemfibrozil deuterated derivative in treatment of hyperlipidemia. The gemfibrozil deuterated derivative has significantly improved pharmacological effect and significantly reduced toxic metabolites.
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