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Preparation method of monofunctionalized nonlinear polyethylene glycol

A kind of polyethylene glycol, non-linear technology, applied in the field of preparation of monofunctional nonlinear polyethylene glycol, can solve the problem of end group modification rate (substitution rate, functionalization rate limitation, separation and purification difficulty, large molecular weight, etc.

Active Publication Date: 2022-08-02
XIAMEN SINOPEG BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In the above preparation method, two-arm branched polyethylene glycol carboxylic acid is first prepared, and then in the last step, a single reactive group succinimide active ester group is obtained by modifying the terminal carboxyl group; in the process, due to being The modified end group is embedded by two polymer chains, the steric hindrance and other factors lead to the limitation of the modification rate (substitution rate, functionalization rate) of the end group; and because the molecular weight of the end group before and after modification is relatively large, giving The separation and purification of products brings difficulties

Method used

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  • Preparation method of monofunctionalized nonlinear polyethylene glycol
  • Preparation method of monofunctionalized nonlinear polyethylene glycol
  • Preparation method of monofunctionalized nonlinear polyethylene glycol

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preparation example Construction

[0134] The present invention provides a method for preparing a monofunctional nonlinear polyethylene glycol. The general structural formula (design structure) of the monofunctional nonlinear polyethylene glycol is shown in formula (1):

[0135] Among them, F is a functional group, which contains a functional end group R 01 ;R 01 with L d Directly connected, or through a divalent linking group Z and L d connected;

[0136] L d is a covalent linking group containing a heteroatom; and L d Contains a covalent linker that can be formed by a coupling reaction, or L d It forms a covalent linking group with U that can be generated through a coupling reaction.

[0137] L d Not only can it contain conventional divalent linking groups such as amide bonds, ester bonds, and carbamate bonds, but also non-linear linking groups such as three-carbon bridges, such as functional groups B5, B6, E13 and disulfide bond. base, such as reacting with the disulfide bond in the five-membered r...

Embodiment 1

[0286] The monofunctionalized nonlinear polyethylene glycol derivatives of Example 1 and Example 2 can also be attributed as follows: XPEG has the general formula mPEG, and two L xBoth -CH 2 CH 2 OCONH- (the number of atomic spacers is 5), U is -(-CH 2 CH 2 CH 2 CH 2 ) CH-, L in embodiment 1 d Contains -CONH- and -NHCO-, F is -CH 2 CH 2 -MAL (wherein MAL is maleimide group), L of Example 2 d Contains -CONH-, F is -CH 2 CH 2 -CHO. The above two embodiments can also be attributed as follows: two L x both -CH 2 CH 2 OCONH- (the number of atomic spacers is 5) and -CH 2 CH 2 OCONH(CH 2 ) 4 - (the number of atomic spacers is 9), and U is >CH-. It can also be attributed as follows: XPEGs all have the general formula mPEG-CH 2 CH 2 -, L x Both are -OCONH- (the number of atomic spacers is 3), and U is -(-CH 2 CH 2 CH 2 CH 2 )CH-; or two L x are -OCONH- (the number of atomic spacers is 3) and -OCONH (CH 2 ) 4 - (the number of atomic spacers is 7), and U is >C...

Embodiment 7

[0288] In Example 7, two L x Both -CH 2 CH 2 COO-.

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Abstract

The invention discloses a preparation method of monofunctional nonlinear polyethylene glycol. The monofunctionalized nonlinear polyethylene glycol has a nonlinear multivalent group U, one side is connected with a single functional end group, and the other side is connected with at least two linear polyethylene glycol chains. The present invention: the first step is to obtain a low-molecular-weight intermediate IM1, and introduce a single functional end group or its slightly modified form; this step only involves the organic reaction between low-molecular-weight reagents, has good controllability, and can precisely control the structure, There are various separation methods to choose from, and high-purity intermediates can be obtained; the polyethylene glycol component can be introduced in the second step, which can be directly obtained or can be obtained by simple chemical modification of the terminal. Ethylene Glycol. When the functional modification is continued or the multi-level branched nonlinear structure is used as a reaction raw material, the reaction steric hindrance is small, and a relatively high substitution rate or grafting rate can also be obtained.

Description

technical field [0001] The invention relates to the field of polymer synthesis, in particular to a preparation method of monofunctionalized nonlinear polyethylene glycol. Background technique [0002] PEGylation is one of the important means of drug modification. Among them, functionalized polyethylene glycol (PEG) can utilize the active groups it contains to interact with drug molecules (including protein drugs and organic small molecule drugs), peptides, carbohydrates, lipids, oligonucleotides, affinity ligands The PEGylation of drugs and other biologically related substances can be achieved by coupling covalent bonds with liposomes, cofactors, liposomes, and biological materials. The modified drug molecule will have many excellent properties of polyethylene glycol, such as hydrophilicity, flexibility, anticoagulant and so on. In addition, due to the steric exclusion effect, PEG-modified drugs can avoid glomerular filtration and biological reactions such as immune respon...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G65/336C08G65/333C08G65/334
CPCC08G65/336C08G65/33396C08G65/3348C08G2650/30C08G2650/04C08G2650/38C08G2650/50C08G2650/60
Inventor 翁文桂刘超闫策王爱兰周纯
Owner XIAMEN SINOPEG BIOTECH
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