Photosensitizer based on 1, 8-naphthalimide and phototherapy application thereof

By optimizing the synthesis path of 1,8-naphthalene lactimide photosensitizer, the problems of insufficient light penetration depth and poor water solubility are solved, efficient reactive oxygen production and tumor targeting are achieved, and the effect of photodynamic therapy is improved.

CN120247943AActive Publication Date: 2025-07-04SHEN ZHEN WAN ZHI DA QI YE GUAN LI YOU XIAN GONG SI
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Patent Information

Application Number
CN202510383504.4
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-03-28
Publication Date
2025-07-04
Estimated Expiration
2045-03-28

AI Technical Summary

Technical Problem

In photodynamic therapy, existing 1,8-naphthalene lactimide photosensitizers have problems such as insufficient light penetration depth, poor tumor tissue targeting and low singlet oxygen quantum yield, and some compounds have poor water solubility, which affects their transmission and distribution in biological bodies.

Method used

By synthesizing a photosensitizer based on 1,8-naphthalene lactimide, using specific synthesis pathways and reaction conditions, including the use of phosphorus oxychloride and boron trifluoride ether complex for fluoroboration, the compounds Np-BOP, Np-OMe and Np-OEt were obtained, and the feed sequence and proportion were optimized to ensure that the reaction was complete and there were few side reactions.

Benefits of technology

The photosensitizer is able to efficiently produce reactive oxygen species under specific wavelengths of light, showing significant phototoxicity and selective accumulation of tumor cells, improving the safety and selectivity of phototherapy, having good photostability and modifyability, and is suitable for tumor targeted treatment.

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Abstract

The invention discloses a photosensitizer based on 1, 8-naphthalimide and phototherapy application thereof.The photosensitizer is obtained by taking 1, 8-naphthalimide and acetylpyrrole as raw materials through phosphorus oxychloride condensation and then fluoroborization, the synthesis method is very simple, and separation and purification are convenient. The compound has the characteristic of long wavelength absorption due to the expanded conjugated structure, and the optical characteristic enables the compound to be effectively applied to the field of photodynamic therapy.
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