Method of preparing branched polyethylene glycol

A polyethylene glycol and branched technology, which is applied in the fields of biomedicine and protein chemistry, can solve the problems of biodegradation, difficult control of reaction conditions, high price of branched polyethylene glycol, etc., and achieves high yield and high price. cheap effect

Inactive Publication Date: 2006-05-03
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

These defects include: 1. rapid elimination, 2. biodegradation, 3. immune response, etc.
[0014] The disadvantage is that although the yield is high, the reaction conditions are difficult to control;
[0015] The above-mentioned defect of above-mentioned synthetic method causes the product price of branched polyethylene glycol, limits the application of branched polyethylene glycol to a large extent in research and practice

Method used

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  • Method of preparing branched polyethylene glycol
  • Method of preparing branched polyethylene glycol
  • Method of preparing branched polyethylene glycol

Examples

Experimental program
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Effect test

Embodiment 1

[0043] Embodiment 1, prepare a kind of branched polyethylene glycol with the method of the present invention, its step is:

[0044] 1. Preparation of lysine ethyl ester hydrochloride

[0045] Dissolve L-lysine in absolute ethanol, feed dry hydrogen chloride gas to saturation under stirring conditions, heat to reflux to dissolve L-lysine, and leave the solution overnight; then distill under reduced pressure to remove excess ethanol and hydrogen chloride ; Finally, carry out crystallization of ethyl lysine hydrochloride with anhydrous ether; then filter, wash, and dry to obtain light yellow crystals of ethyl lysine hydrochloride;

[0046] 2, the preparation molecular weight is the carboxymethylated monomethoxy polyethylene glycol of 5000

[0047] Dissolve mPEG5000 in dry dichloromethane, add activated manganese dioxide, mix evenly, and stir overnight at room temperature; filter to remove the catalyst, and evaporate the solvent under reduced pressure to obtain an intermediate ox...

Embodiment 2

[0054] Embodiment 2, prepare a kind of branched polyethylene glycol with the method of the present invention, its step is:

[0055] 1. Preparation of lysine ethyl ester hydrochloride

[0056] Dissolve L-lysine in absolute ethanol (1:8 molar ratio), feed dry hydrogen chloride gas to saturation under stirring conditions, heat to reflux to dissolve L-lysine, and leave the solution overnight; then reduce Pressure distillation removes excess ethanol and hydrogen chloride; Finally, carry out the crystallization of ethyl lysine hydrochloride with anhydrous ether; then filter, wash, and dry to obtain light yellow crystals of ethyl lysine hydrochloride;

[0057] 2. Preparation of molecular weight is 2000 carboxymethylated monomethoxypolyethylene glycol

[0058] Dissolve 25 grams of mPEG2000 in dry dichloromethane, add 20 grams of activated manganese dioxide, mix uniformly, and stir overnight at room temperature; filter to remove the catalyst, and evaporate the solvent under reduced pr...

Embodiment 3

[0065] Embodiment 3, prepare a kind of branched polyethylene glycol with the method of the present invention, its step is:

[0066] 1. Preparation of lysine ethyl ester hydrochloride

[0067] Dissolve L-lysine in absolute ethanol, feed dry hydrogen chloride gas to saturation under stirring conditions, heat to reflux to dissolve L-lysine, and leave the solution overnight; then distill under reduced pressure to remove excess ethanol and hydrogen chloride ; Finally, carry out crystallization of ethyl lysine hydrochloride with anhydrous ether; then filter, wash, and dry to obtain light yellow crystals of ethyl lysine hydrochloride;

[0068] 2. Preparation of molecular weight is 750 carboxymethylated monomethoxypolyethylene glycol

[0069] Dissolve mPEG750 in dry dichloromethane, add activated manganese dioxide, mix evenly, and stir overnight at room temperature; filter to remove the catalyst, and evaporate the solvent under reduced pressure to obtain an intermediate oxidation pro...

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Abstract

The method for preparing branched polyethylene glycol provided by the invention, the steps are as follows: first prepare lysine ethyl ester hydrochloride and carboxymethylated monomethoxypolyethylene glycol respectively, and mix them uniformly , and then add TEA, DCC, NHS in turn, after deprotection of the product obtained from the reaction, and then separated by gel filtration, branched polyethylene glycol can be obtained. Branched polyethylene glycol is widely used to modify proteins Such as macromolecules, small molecule drugs and surfaces can also be modified; the method of the present invention is simple and easy to operate, and only needs to protect the carboxyl of lysine, and does not need activated amino and carboxyl groups; the reaction is carried out at room temperature without controlling the pH value ; The raw materials and reagents used are cheap; the yield is as high as about 65%.

Description

technical field [0001] The invention belongs to the fields of biomedicine and protein chemistry, in particular to a method for preparing branched polyethylene glycol. Background technique [0002] With the rapid development of biotechnology, more and more peptides, proteins, and enzymes with biological activity are used in clinical treatment. However, these biomacromolecules have some defects when they are directly applied to the human body. These defects include: 1. rapid elimination, 2. biodegradation, 3. immune response and so on. Therefore, the chemical modification of proteins, especially pharmaceutical proteins, is still a hot research field. Many natural and synthetic molecules are being used as chemical modifications. Polyethylene glycol, a synthetic molecule, is widely used in the modification of proteins, polypeptides, enzymes and even some small molecule drugs due to its biocompatibility, non-toxicity to the human body, and the abili...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G65/34
Inventor 苏志国何明磊
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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