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Polyoxyethylene ligand containing coupler and its synthesis process

A technology of polyoxyethylene and synthetic methods, which is applied in the fields of medical science and chemical synthesis, can solve the problems of long half-life and high relaxation rate, and achieve the effect of long half-life, high relaxation rate, and not easy to adhere to the blood vessel wall

Inactive Publication Date: 2006-10-18
EAST CHINA NORMAL UNIVERSITY
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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: crude polyoxyethylene ligand containing coupling agent

[0042] Into the reactor, add 28 mg of amine-terminated polyoxyethylene-diethylenetriaminepentaacetic acid block polymer, 2.5 ml of solvent N,N-dimethylformamide, and coupling agent 3-maleamide benzoic acid-N- Succinimidyl ester (MBS) 3.8mg, reacted at room temperature for 0.5 hours, amine-terminated polyoxyethylene-diethylenetriaminepentaacetic acid block polymer, solvent N,N-dimethylformamide, coupling agent 3 -The weight ratio of maleamide benzoic acid-N-succinimidyl 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 represents 45;

[0047]The crude product of polyoxyethylene ligand containing coupling agent is obtained, and has the following structur...

Embodiment 2

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

[0058] Into the reactor, add 99 mg of amine-terminated polyoxyethylene-diethylenetriaminepentaacetic acid block polymer, 3 ml of solvent N,N-dimethylformamide, and coupling agent 3-maleamide benzoic acid-N-hydroxyl Succinimidyl ester (MBS) 6.0 mg, 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 and 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 is to prepare the refined product of the polyoxyethylene ligand containing the coupling agent

[0061] ...

Embodiment 3

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

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

[0066] The second step is to prepare the refined product of the polyoxyethylene ligand containing the coupling agent

[0067] Water was added, dialyzed, and freeze-dried to obtai...

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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 method for synthesizing the above-mentioned polyoxyethylene ligand containing a coupling agent, belonging to the technical fields of medical science and chemical synthesis. Background technique [0002] In the field of life sciences, more scientific detection and tracking methods are needed in terms of whether targeted peptides and targeted drugs are targeted to special organs or lesions, and the early safety assessment of gene therapy methods. It is widely adopted because MRI can detect tracking without killing experimental animals and tracking for a long time. Therefore, on the one hand, a ...

Claims

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Application Information

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IPC IPC(8): C08G65/333A61K47/34A61K49/22
Inventor 宋春梅庄小璐薛海丽
Owner EAST CHINA NORMAL UNIVERSITY