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Molecularly targeted aza aromatic ring axially substituted phthalocyanine complex and preparation method thereof

A heteroaromatic ring, molecular targeting technology, applied in medical preparations containing active ingredients, pharmaceutical formulations, silicon organic compounds, etc., can solve the problems of poor selectivity, high toxicity, etc. Beneficial to industrial production

Active Publication Date: 2016-12-21
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Molecular targeted therapy has been a hot spot in oncology research in recent years, among which molecular target drugs have attracted much attention. It refers to the use of molecular biological differences between tumor cells and normal cells to inhibit the growth and reproduction of tumor cells, and finally A class of drugs that caused its death. For a long time, in order to overcome the disadvantages of poor selectivity and high toxicity of cytotoxic anti-tumor drugs, researchers have been working hard to find drugs that can specifically recognize and kill tumor cells

Method used

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  • Molecularly targeted aza aromatic ring axially substituted phthalocyanine complex and preparation method thereof
  • Molecularly targeted aza aromatic ring axially substituted phthalocyanine complex and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 (M=Si, n=4)

[0028] (1) Add 23.29 g (0.12 mol) of tetraethylene glycol and 15.18 g (0.15 mol) of triethylamine in sequence into a 250 mL round bottom flask equipped with a magnetic stirring device, an air duct device and a reflux condensing device and 50 mL of dichloromethane, then dissolve 5.72 g (0.03 mol) of p-toluenesulfonyl chloride in 100 mL of dichloromethane, and install it in a constant pressure dropping funnel, slowly drop the p-toluenesulfonyl chloride solution under nitrogen protection Added to the reaction flask, then stirred at room temperature for 8 h. After the reaction was finished, extract three times with 1 mol / L hydrochloric acid solution and saturated sodium chloride solution respectively, collect the organic layer, and then remove dichloromethane by distillation under reduced pressure; The developer is a mixed solution of petroleum ether: ethyl acetate = 1:1, and about 8.35 g of light yellow viscous liquid (ie compound 2a) is obtained, ...

Embodiment 2

[0032] Example 2 (M=Si, n=5)

[0033] (1) Add 10.76 g (0.12 mol) pentaethylene glycol, 4.57 g (0.15 mol) triethylamine and 50 mL Dichloromethane, then dissolve 2.15g (0.03 mol) p-toluenesulfonyl chloride in 100 mL of dichloromethane, and install it in a constant pressure dropping funnel, and slowly drop the p-toluenesulfonyl chloride solution to the reaction under nitrogen protection bottle, and then stirred at room temperature for 10 h. After the reaction was finished, extract three times with 1 mol / L hydrochloric acid solution and saturated sodium chloride solution respectively, collect the organic layer, and then remove dichloromethane by distillation under reduced pressure; The developer is a mixed solution of petroleum ether: ethyl acetate = 1:1, and about 6.15 g of a light yellow viscous liquid (compound 2b) is obtained, with a yield of 83%;

[0034] (2) Add 1.01 g (4.50 mmol) N-(3-chloro-4-fluorophenyl)-7-methoxy to a 100 mL round bottom flask equipped with a magnetic...

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Abstract

The invention discloses a molecularly targeted aza aromatic ring axially substituted phthalocyanine complex and a preparation method thereof. The molecular target drug N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholine-4-propoxy)quinazoline-4-amine with an alkoxy long chain is introduced to the axial direction of a phthalocyanine large ring so as to increase its amphipathy, biocompatibility and photosensitizer targeting. The compound has the advantages of single structure, definite composition, no isomer, and easy product purification, also the complex is not easy to gather, thus being conducive to increasing the cell uptake rate. The synthesis method of the complex provided by the invention is simple, and has the characteristics of few side reaction, easily available raw materials, and low cost, and is in favor of industrial production.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a molecularly targeted azaaromatic ring axially substituted phthalocyanine complex and a preparation method thereof. Background technique [0002] At present, there are many cancer treatment methods, and photodynamic therapy has gradually become a hot research field because of its unique advantages. Photodynamic therapy refers to the use of photosensitizers to generate photodynamic effects under the excitation of light of a certain wavelength to diagnose and treat diseases. [0003] Its action process is to inject a certain dose of photosensitizer into the human body. After a certain period of time, the photosensitizer is selectively enriched in the diseased tissue to a certain extent, and then the diseased tissue is irradiated with light of a certain wavelength, and the photosensitizer will be stimulated by light. A series of photophysical and photochemical reacti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/22C07F7/02A61K41/00A61P35/00
CPCA61K41/0071C07D487/22C07F7/025
Inventor 薛金萍陈涓涓黄逸臻
Owner FUZHOU UNIV
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