An isopulegol bisdifluoroalkylated derivative having anticancer activity, and a preparation method and application thereof

CN122145336APending Publication Date: 2026-06-05SHANGHAI JIAOTONG UNIV

Patent Information

Authority / Receiving Office: CN · China
Patent Type: Applications(China)
Current Assignee / Owner: SHANGHAI JIAOTONG UNIV
Filing Date: 2026-02-06
Publication Date: 2026-06-05

AI Technical Summary

Technical Problem

The difluoroalkylation reaction of isoprene has not been effectively achieved in the existing technology, which limits its application in the field of anti-tumor drugs. Furthermore, the existing methods have low reaction efficiency and poor selectivity, making it difficult to advance the research and development of anti-tumor drugs.

Method used

A photocobalt-cobalt synergistic catalytic iterative addition-elimination strategy was adopted to achieve the difluoroalkylation of isoprene by reacting a halodifluoroamide reagent with isoprene under photocobalt synergistic catalysis via lanthanum(III) trifluoromethanesulfonate catalysis.

Benefits of technology

The drug molecule isopleleol was successfully modified into a drug molecule with good anti-breast cancer activity, exhibiting excellent tumor growth inhibition ability and significant anti-tumor activity, providing a basis for the research and development of novel anti-breast cancer drugs, with high yield and good biosafety.

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Abstract

The present application relates to the technical field of pharmaceutical chemistry, and particularly relates to an isopulegol bisdifluoroalkyl derivative with anticancer activity and a preparation method and application thereof. The present application realizes the bisdifluoroalkylation of isopulegol through a light cobalt synergistic catalytic iterative addition elimination strategy, and modifies isopulegol, which has no anti-breast cancer activity, into a drug molecule, i.e. the isopulegol bisdifluoroalkyl derivative, which has good anti-breast cancer activity. The isopulegol bisdifluoroalkyl derivative provided by the present application shows excellent tumor growth inhibition capacity, significant anti-tumor activity and good biological safety, and provides an important technical basis and support for the research and development of a new anti-breast cancer drug, and has a great potential application prospect in the field of tumor treatment.

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