Water-soluble polymer iron chelator as well as preparation method and application thereof

A technology of water-soluble polymerization and chelating agent, used in drug combination, blood diseases, extracellular fluid diseases, etc.

Inactive Publication Date: 2012-07-25
ZHEJIANG GONGSHANG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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  • Water-soluble polymer iron chelator as well as preparation method and application thereof
  • Water-soluble polymer iron chelator as well as preparation method and application thereof
  • Water-soluble polymer iron chelator as well as preparation method and application thereof

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Embodiment 1

[0032] Embodiment 1, a kind of preparation method of polymer chelating agent (1a), the structural formula of this polymer chelating agent is as follows;

[0033]

[0034] Follow the steps in order:

[0035] 1), the synthesis of the benzyl-protected 3-hydroxypyridin-4-one bidentate ligand (8) containing free amino groups (the synthetic route is as follows):

[0036]

[0037] A. Synthesis of benzyl maltol (4):

[0038] Using maltol (3) as raw material, according to literature method (Y.Ma, W.Luo, P.J.Quinn, Z.Liu, and R.C.Hider, Design, Synthesis, Physicochemical Properties, and Evaluation of Novel Iron Chelators with Fluorescent Sensors, J .Med.Chem.2004, 47, 6349-6362) for synthesis;

[0039] Synthesis of B, 3-benzyloxy-1-(2-benzyloxyethyl)-2-methylpyridin-4(1hydrogen)-one (5):

[0040] Take benzyl maltol (4) (10g, 46.3mmol) and dissolve it in 100ml of ethanol, then add 150ml of distilled water and 2-benzyloxyethylamine (17.5g, 116mol), and heat the resulting mixture at...

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Abstract

The invention discloses a water-soluble polymer iron chelator with a structural general formula shown as the specification, wherein R is alkyl from C1 to C3, (CH2)2-6OH, (CH2)2-6OCH3, (CH2CH2O)1-3H or polyhydroxyl group; R' is H or CH3; n is any one integer selected from 2 to 8; X is O or NH; x ranges from 5 to 200; and y ranges from 50 to 2000. The invention also discloses a preparation method and application of the water-soluble polymer iron chelator. The water-soluble polymer iron chelator can be used for preparing medicaments for treating diseases relevant to overhigh iron content or antibacterial drugs for external use and can also be used for preserving cosmetics or foods.

Description

technical field [0001] The invention relates to a class of water-soluble polymer chelating agent and its preparation method and application. The chelating agent has high affinity and selectivity to ferric iron. Background technique [0002] Polymeric chelating agents have been widely used in water treatment, pollution control, metal recovery and analytical chemistry. Recently, the application of polymeric chelating agents in the biomedical field has also been reported. Iron is an essential element for the life processes of all organisms, yet it can be toxic when present in excess in organisms. Therefore, iron chelators have been used to treat diseases associated with excess iron (such as thalassemia, hemochromatosis and other inherited blood diseases). Targeting iron is an effective method for the treatment of microbial infections, and it also has good prospects in the treatment of malaria, tumors, and neurodegenerative diseases (such as Alzheimer's disease, Parkinson's di...

Claims

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Application Information

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IPC IPC(8): C08F220/28C08F222/38A61P7/06A61P7/00A61P31/04
Inventor 周涛罗伯特·查尔斯·海德徐波
Owner ZHEJIANG GONGSHANG UNIVERSITY
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