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Polyoxyethylene ligand containing coupler and its synthesis process

A polyoxyethylene and synthetic method technology, applied in the fields of medical science and chemical synthesis, can solve the problems of high relaxation rate and long half-life, and achieve the effects of high relaxation rate, long half-life and good biocompatibility

Inactive Publication Date: 2008-01-30
EAST CHINA NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In short, so far, there is no ligand that can be made into a key drug or a contrast agent that can simultaneously meet the characteristics of targeting, long half-life, and high relaxation rate.

Method used

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  • Polyoxyethylene ligand containing coupler and its synthesis process
  • Polyoxyethylene ligand containing coupler and its synthesis process
  • Polyoxyethylene ligand containing coupler and its synthesis process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] The first step contains the crude product of polyoxyethylene ligand of coupling agent

[0042] Add 28 mg of amino-terminated polyoxyethylene-diethylenetriaminepentaacetic acid block polymer, 2.5 ml of solvent N, N-dimethylformamide, coupling agent 3-maleamide benzoic acid-N- Succinimide ester (MBS) 3.8 mg, reacted at room temperature for 0.5 hours, amino-terminated polyoxyethylene-diethylenetriaminepentaacetic acid block polymer, solvent N, N-dimethylformamide, coupling agent 3 -The weight ratio of maleamide benzoic acid-N-succinimide ester (MBS) is 1: 89: 0.136, and the structural formula of the amino-terminated polyoxyethylene-diethylenetriaminepentaacetic acid block polymer is

[0043]

[0044] In the formula, R 1 The structural formula representing polyoxyethylene is

[0045] -CH 2 CH 2 -(OCH 2 CH 2 ) n -

[0046] n stands for 45;

[0047] A crude product of polyoxyethylene ligand containing a coupling agent was obtained with the following structure,

...

Embodiment 2

[0057] The first step is to prepare the crude product of polyoxyethylene ligand containing coupling agent

[0058] Add 99mg of amino-terminated polyoxyethylene-diethylenetriaminepentaacetic acid block polymer, 3ml of solvent N,N-dimethylformamide, coupling agent 3-maleamide benzoic acid-N-hydroxy 6.0 mg of succinimide ester (MBS), reacted at room temperature for 2 hours to obtain a crude product of polyoxyethylene ligand containing a coupling agent; amino-terminated polyoxyethylene-diethylenetriaminepentaacetic acid block polymer, The weight ratio of solvent N, N-dimethylformamide, coupling agent 3-maleamide benzoic acid-N-hydroxysuccinimide ester (MBS) is 1: 30.3: 0.061; R in the structural formula of diethylenetriaminepentaacetic acid block polymer 1 represent

[0059] -CH 2 CH 2 -(OCH 2 CH 2 ) n -, n represents 113;

[0060] The second step prepares the refined product containing the polyoxyethylene ligand of coupling agent

[0061] Add water, dialyze, and freeze-d...

Embodiment 3

[0064] The first step is to prepare the crude product of polyoxyethylene ligand containing coupling agent

[0065] Add 99 mg of amino-terminated polyoxyethylene-diethylenetriaminepentaacetic acid block polymer, 1 ml of phosphoric acid PBS buffer solvent, and coupling agent 3-maleamide benzoic acid-N-hydroxysuccinimide ester into the reactor (MBS) 6.0 mg, reacted at room temperature for 24 hours to obtain a crude product of polyoxyethylene ligand containing a coupling agent; amino-terminated polyoxyethylene-diethylenetriaminepentaacetic acid block polymer, solvent phosphoric acid PBS buffer solvent , The weight ratio of coupling agent 3-maleamide benzoic acid-N-hydroxysuccinimide ester (MBS) is 1: 10.1: 0.061; Same as embodiment 2;

[0066] The second step prepares the refined product containing the polyoxyethylene ligand of coupling agent

[0067] Add water, dialyze, and freeze-dry to obtain 90 mg of refined polyoxyethylene ligand containing coupling agent, and the product y...

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Abstract

The present invention belongs to the field of medicine and chemical synthesis technology, and is polyoxyethylene ligand containing coupling agent and its synthesis process. The polyoxyethylene ligand is prepared through reaction of amino-terminated polyoxyethylene-diethylenetriamine pentaacetic acid block polymer, solvent and coupling agent in certain weight proportion at -4 deg.c to room temperature for 0.5-72 hr to obtain coarse product of polyoxyethylene ligand containing coupling agent; dialyzing and freeze drying the coarse product to obtain white powdered product of polyoxyethylene ligand containing coupling agent. The present invention has simple product synthesis and purification and high yield, and the product is used in preparing contrast agent for intravenous injection, magnetic resonance imaging, etc.

Description

technical field [0001] The invention relates to a polyoxyethylene ligand containing a coupling agent. The ligand can react with various targeting drug polypeptides, proteins, DNA and western medicines through terminal functional groups to prepare targeted drugs, and can also be directly made into contrast agents. . The present invention further relates to a synthesis method of the polyoxyethylene ligand containing a coupling agent, which belongs to the technical fields of medical science and chemical synthesis. Background technique [0002] In the field of life sciences, whether targeted peptides and targeted drugs are targeted to special organs or lesion sites, and early safety assessment of gene therapy methods require more scientific detection and tracking methods. Since the detection and tracking of magnetic resonance imaging can be widely used without killing experimental animals and tracking for a long time. Therefore, on the one hand, contrast agents with targeting,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G65/333A61K47/34A61K49/22
Inventor 宋春梅庄小璐薛海丽
Owner EAST CHINA NORMAL UNIV
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