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A kind of photosensitizer, preparation method and application thereof

A photosensitizer and coupling reaction technology, applied in photodynamic therapy, chemical instruments and methods, pharmaceutical formulations, etc., can solve the problems of poor treatment effect, high toxicity to human body, and difficult to synthesize, and achieve improved effect and high molar extinction coefficient. , the effect of reducing biological toxicity

Active Publication Date: 2019-04-12
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In view of this, the present invention provides a photosensitizer, a preparation method and its application, which solves the technical problems that the existing photosensitizers have poor therapeutic effect, are highly toxic to the human body, are expensive and difficult to synthesize

Method used

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  • A kind of photosensitizer, preparation method and application thereof
  • A kind of photosensitizer, preparation method and application thereof
  • A kind of photosensitizer, preparation method and application thereof

Examples

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Embodiment 1

[0028] Step 1: Dissolve selenophene (1.0 g, 7.6 mmol) in chloroform (10 mL), under nitrogen protection, add NBS into the reaction system, and stir the mixture at room temperature for one day. After the reaction is over, add deionized water to quench the reaction, extract with dichloromethane, add saturated sodium thiosulfate solution and deionized water to wash respectively, dry with anhydrous sodium sulfate, spin dry the solvent, and use pure petroleum Carry out column chromatography purification with ether as developing agent, obtain light green liquid 1.852g, promptly obtain Determining its productive rate is 84.4%, and its nuclear magnetic data is 1 H NMR(400MHz,Chloroform-d)δ7.00(s,2H).

[0029] Step 2: Put (3.46mmol, 1.0g), cuprous iodide (0.692mmol, 0.131g), bistriphenylphosphine palladium dichloride (0.346mmol, 0.242g) dissolved in triethylamine (10mL) / THF (20mL) In the mixed solution, under the protection of nitrogen, trimethylsilylethynyl (17.3mmol, 1.18mL) was ...

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Abstract

The invention belongs to the technical field of light power treatment, and more specifically relates to a photosensitizer, and a preparation method and applications thereof. The photosensitizer is a compound with a structure represented by formula I. According to the preparation method, a compound with a structure represented by formula II and a compound with a structure represented by formula IIIare subjected to sonogashira coupling reaction so as to obtain the compound with a structure represented by formula I. The preparation method is capable of solving problems in the prior art that conventional photosensitizers are poor in treatment effect, the toxicity on human body is large, cost is high, and synthesis is inconvenient to realize.

Description

technical field [0001] The invention relates to the technical field of photodynamic therapy, in particular to a photosensitizer, a preparation method and an application thereof. Background technique [0002] Photodynamic therapy is a method of treating cancer in a non-surgical way. It uses photosensitizers to absorb photons under light conditions to reach the excited state, and then reach the triplet state through intersystem crossing. A triplet-triplet energy transfer process occurs, and the energy is transferred to oxygen to obtain singlet oxygen to kill cancer cells. Therefore, designing and synthesizing a photosensitizer with excellent performance is particularly important for photodynamic therapy. [0003] At present, the photosensitizers used in photodynamic therapy are mostly transition metal complexes, photosensitizers substituted by iodine atoms or bromine atoms, etc., which use transition metals, iodine or bromine atoms to exert heavy atom effects to promote inters...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F5/02A61K41/00A61P35/00
CPCA61K41/0057A61P35/00C07F5/022
Inventor 籍少敏林丹梁辉霍延平董玉叶
Owner GUANGDONG UNIV OF TECH
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