Branching poly-ethylene and its production

A polyethylene glycol and branched technology, applied in the field of branched polyethylene glycol and its preparation, to achieve the effects of reducing the generation of isomers, reducing the loss of biological activity, and reducing the steric hindrance effect

Inactive Publication Date: 2007-09-05
NAT UNIV OF DEFENSE TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As a common group of polyethylene glycol derivatives, maleimide has been widely used in the modification of proteins or polypeptides, but so far, the related modifiers are linear polyethylene glycol. Among branched polyethylene glycol modifiers, no reports have been seen

Method used

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  • Branching poly-ethylene and its production
  • Branching poly-ethylene and its production
  • Branching poly-ethylene and its production

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] 1.Fmoc-Glu-(mPEG 750 ) 2 Preparation

[0030] Respectively 3.7 grams of Fmoc-Glu, 22.5 grams of monomethoxy polyethylene glycol (mPEG) with a molecular weight of 750 750 ) And 0.9 g of DMAP are placed in a long-necked flask, add 100 ml of analytically pure dichloromethane and 10 ml of analytically pure tetrahydrofuran, put in a magnet, stir at room temperature to dissolve the reactants, 10 minutes later, add 8.0 grams of DCC, The reaction was stirred at 0°C for 24 hours. After the reaction, the temperature control was stopped, and the temperature was raised to room temperature. The reaction was continued for 1 hour. After removing the white precipitate by filtration, 4.0 g of oxalic acid was added, and the reaction was stirred at room temperature for 1 hour. After filtration, the filtrate was concentrated to 20 by rotary evaporation at a temperature of 45°C. After 1 milliliter, it was naturally cooled to room temperature, 200 milliliters of anhydrous ether was added, and th...

Embodiment 2

[0039] 1.Fmoc-Glu-(mPEG 2000 ) 2 Preparation

[0040] Respectively, 4.1 grams of Fmoc-Glu and 60.0 grams of monomethoxy polyethylene glycol (mPEG) with a molecular weight of 2000 2000 ) And 0.8 g of DMAP are placed in a long-necked flask, add 150 ml of analytically pure dichloromethane and 15 ml of analytically pure tetrahydrofuran, put in a magnet, and stir at room temperature to dissolve the reactants. After 15 minutes, add 6.0 grams of DCC. The reaction was stirred at 5°C for 26 hours. After the completion of the reaction, the temperature control was stopped, the temperature was raised to room temperature naturally, and the reaction was continued with stirring for 1 hour. After the white precipitate was removed by filtration, 3.2 g of oxalic acid was added, the reaction was stirred at room temperature for 1 hour, filtered, and the filtrate was concentrated to 30 ml by rotary evaporation at a temperature of 45° C., and then naturally cooled to room temperature, 300 ml of anhydro...

Embodiment 3

[0049] 1.Fmoc-Glu-(mPEG 5000 ) 2 Preparation

[0050] Respectively 4.4 grams of Fmoc-Glu, 150.0 grams of monomethoxy polyethylene glycol (mPEG) with a molecular weight of 5000 5000 ) And 0.7 g of DMAP are placed in a long-necked flask, add 300 ml of analytically pure dichloromethane and 30 ml of analytically pure tetrahydrofuran, put in a magnet, and stir at room temperature to dissolve the reactants. After 20 minutes, add 7.2 grams of DCC. The reaction was stirred at -5°C for 30 hours. After the completion of the reaction, the temperature control was stopped, the temperature was raised to room temperature naturally, and the reaction was continued with stirring for 1 hour. After the white precipitate was removed by filtration, 3.5 g of oxalic acid was added, the reaction was stirred at room temperature for 1 hour, filtered, and the filtrate was concentrated to 50 ml by rotary evaporation at a temperature of 45°C, and then naturally cooled to room temperature, 500 ml of anhydrous e...

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Abstract

Production of branched polyglycol consists of four steps: preparing branched polyglycol with glutamic acid of 9-fluorenmethoxy-oxo- protecting amino as central molecule, preparing branched polyglycol with glutamic acid as central molecule, preparing maleimide and preparing the final product. In the structural formula, n is >=1, and m is between 4-500. It can modify protein and polypeptide, decrease biological activity and hindering effect.

Description

Technical field [0001] The invention relates to a branched polyethylene glycol and a preparation method thereof. Background technique [0002] In the field of drug delivery today, polyethylene glycol modification (PEGylation, PEGylation, PEGylation) is an important method that is widely used, especially in improving the clinical application of protein and peptide drugs. One of the successful technologies (J. Clin. Pharmacokinet, 2000, 40: 539; J. Adv. Drug Deliv. Rev., 1993, 10: 91; J. Eur. J. Pharm. Biopharm., 2004, 58: 185 ). However, this technology still has some problems in practical applications, which are mainly manifested in the fact that the biological activity of protein drugs is greatly reduced after PEGylation. However, recent studies have shown that when a PEG with a special structure is used for modification, the activity loss of the modified drug can be significantly reduced. This PEG with a special structure is called a branched PEG (Branched PEG). Compared with l...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/48A61K47/34A61K47/10
Inventor 李效东刘克良王孝杰
Owner NAT UNIV OF DEFENSE TECH
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