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

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

Inactive Publication Date: 2014-03-05
ZHEJIANG GONGSHANG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

There are few reports about water-soluble polymer iron chelating agents

Method used

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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 preparation method of polymer chelating agent (1a), the structural formula of the polymer chelating agent is as follows;

[0033]

[0034] Follow these steps in sequence:

[0035] 1) Synthesis of 3-hydroxypyridin-4-one bidentate ligand (8) with free amino group-protected benzyl group (the synthesis route is as follows):

[0036]

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

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

[0039] B. Synthesis of 3-benzyloxy-1-(2-benzyloxyethyl)-2-methylpyridine-4(1hydro)-one (5):

[0040] Take benzyl maltol (4) (10g, 46.3mmol) dissolved in 100ml of ethanol, then add 150ml of distilled water, 2-benzyloxyethylamine (17.5g, 116mol), and heat the resulting mixture at 130°C Reflux for 16 hours. Rotary ev...

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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 type of water-soluble polymer chelating agent, and a preparation method and application thereof. The chelating agent has high affinity and selectivity for trivalent iron. Background technique [0002] Polymer chelating agents have been widely used in water treatment, pollution control, metal recovery and analytical chemistry. Recently, the application of polymer chelating agents in the field of biomedicine has also been reported. Iron is an essential element in the life process of all living things, but when it exists in the living body too much, it can produce toxicity. Therefore, iron chelators have been used to treat diseases related to excessive iron (such as thalassemia, hemochromatosis and other inherited blood diseases). Iron as a target is an effective method to treat microbial infections, and it also has a good prospect in the treatment of malaria, tumors, and neurodegenerative diseases (such as Alzheimer's disease, Par...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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