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Axial substituted phthalocyanine compound, its preparation and application in optical kinetic treatment

A complex and axial technology, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, and compounds containing elements of Group 3/13 of the periodic table, etc., which can solve the problems of complex synthesis and high cost , to achieve the effects of strong photosensitization ability, no isomers, and simple preparation

Inactive Publication Date: 2005-02-23
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the synthesis of Pc4 is relatively complicated and costly. More importantly, Pc4 is not a drug with independent intellectual property rights in my country.

Method used

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  • Axial substituted phthalocyanine compound, its preparation and application in optical kinetic treatment
  • Axial substituted phthalocyanine compound, its preparation and application in optical kinetic treatment
  • Axial substituted phthalocyanine compound, its preparation and application in optical kinetic treatment

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preparation example Construction

[0043] 2. The preparation method of the new axially substituted phthalocyanine complex of the present invention comprises the following major steps: (a) dichlorosilicon phthalocyanine (or a chloroaluminum phthalocyanine) and the corresponding The reactants are dispersed in a suitable solvent according to a certain molar ratio of feed; (b) in the presence of sodium hydride or potassium carbonate, reflux reaction for 1 hour to 3 days, and monitor the reaction end point by chromatography; (c) by solvent method And / or chromatography to remove excess raw materials and impurities and purify the target product. For the schematic diagram of the reaction, please refer to the attached Figure 19 , 20 .

[0044] The corresponding reactants containing substituents described in the present invention include: sulfamic acid; Glucose; Diethylene glycol butyl ether; 4-ethyl phenol; 4-butyl phenol; 4-aminophenol; 2-ethoxy-4-formylphenol; 2-dimethylaminoethanol; 3-diethylaminophenol; pyrimidi...

Embodiment 1

[0048] Stir 0.1g of dichlorosilicon phthalocyanine, 0.3g of sulfamic acid, and 20mg of NaH in 10ml of toluene, reflux for 3 days, remove the solvent by rotary evaporation under reduced pressure, add 100ml of water to the solid, filter, and dissolve the filter cake with dichloromethane, pass Silica gel chromatography column separation and purification, the eluent was ethanol, and after vacuum drying, dark blue bis(aminosulfonyl)silyl phthalocyanine was obtained with a yield of 38.3%.

Embodiment 2

[0050] Stir 0.1g of dichlorosilicon phthalocyanine, 10ml of diethylene glycol butyl ether, and 20mg of NaH in 10ml of toluene, reflux for 3 days, remove the solvent by rotary evaporation under reduced pressure, add 100ml of water to the solid, filter, and dissolve the filter cake with dichloromethane , separated and purified by silica gel chromatography, the eluent is chloroform. After vacuum drying, dark blue bis(2-(2-butoxyethoxy)ethoxysilylphthalocyanine was obtained with a yield of 21.2%.

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Abstract

An axial substituted phthalocyanine complex, its manufacture and applications in optical dynamics therapy are disclosed. It is prepared by: refluxing silicon dichloride phthalocyanine and monoaluminium phthalocyanine with substitutes contained appropriate compounds and sodium hydrogen or potassium carbonate in appropriate solvent for a certain time, washing with solvent, separating through liquid chromatography, and purifying to obtain products. The complex is prepared simply and quickly, uneasy to be agglomerated, strong optical sensitive, valuble as a drug in optical dynamic treatment. Its structure is clear without isomer.

Description

Technical field: [0001] The present invention relates to an axially substituted phthalocyanine complex, its preparation method and its application in photodynamic therapy. Background technique: [0002] Photodynamic therapy (Photodynamic Therapy), in essence, is the application of the photosensitization reaction of photosensitizers in the medical field. The process of photodynamic therapy is to first inject the photosensitizer into the body, and after a period of time (this waiting time is to allow the drug to be relatively enriched in the target body), the target body is irradiated with light of a specific wavelength (for the target body in the body cavity). The light source can be introduced by means of interventional technology such as optical fiber), and the photosensitizer enriched in the target body is excited by light, which inspires a series of photophysical and photochemical reactions, generates active oxygen, and then destroys the target body (such as cancer cells ...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K47/54A61P35/00C07D487/22C07F5/06C07F7/02
Inventor 黄剑东黄金陵陈耐生张国才
Owner FUZHOU UNIV
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