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Preparation method for Y-type branched hydrophilic polymer carboxylic acid derivative

一种亲水性聚合物、羧酸衍生物的技术，应用在聚合物领域，能够解决产品分离困难、成本高、产率低等问题

Active Publication Date: 2018-10-16
JENKEM TECH CO LTD (LIAONING)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As in the preparation example of CN1243779C, the productive rate of Y-type PEG product is lower, only 50%, product separation difficulty, cost is higher, is unfavorable for industrial amplification

Method used

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  • Preparation method for Y-type branched hydrophilic polymer carboxylic acid derivative
  • Preparation method for Y-type branched hydrophilic polymer carboxylic acid derivative
  • Preparation method for Y-type branched hydrophilic polymer carboxylic acid derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0148] The synthesis (prior art) of the polyethylene glycol-acetic acid (molecular weight 4000) of embodiment 1Y type branch

[0149]

[0150] With reference to the synthetic method of patent CN1243779C embodiment 5, the polyethylene glycol-acetic acid of the Y-type branch that molecular weight is 4000 is prepared: the polyethylene glycol monomethyl ether-aminoacetic acid (mPEG-Gly) that 10g molecular weight is 2000 and 10g molecular weight are 2000 polyethylene glycol monomethyl ether-succinimide carboxyacetate (mPEG-OCH 2 CO-NHS) was dissolved in 200ml of dichloromethane, 2.5ml of triethylamine was added to the solution, reacted overnight at room temperature, the solvent was concentrated by rotary evaporation, the residue was added with diethyl ether, the precipitate was collected by filtration, dried in vacuo, purified by ion exchange chromatography, gel Filter chromatography (GFC) monitoring starts to collect when the peak height of the target product exceeds 5mv, and e...

Embodiment 2

[0164] The synthesis (prior art) of the polyethylene glycol-acetic acid (molecular weight 20000) of embodiment 2Y type branch

[0165] With reference to the synthetic method of patent CN1243779C embodiment 5, the preparation molecular weight is the polyethylene glycol-acetic acid of the Y type branch of 20000: the polyethylene glycol monomethyl ether-aminoacetic acid (mPEG-Gly) that 10g molecular weight is 10000 and 10g molecular weight are 10000 polyethylene glycol monomethyl ether-succinimide carboxyacetate (mPEG-OCH 2 CO-NHS) was dissolved in 200ml of dichloromethane, 0.11ml of triethylamine was added to the solution, reacted overnight at room temperature, the solvent was concentrated by rotary evaporation, the residue was added with diethyl ether, the precipitate was collected by filtration, dried in vacuo, purified by ion exchange chromatography, and monitored by GFC , start to collect when the peak height of the target product exceeds 5mv, and end the collection when it ...

Embodiment 3

[0179] The synthetic (method of the present invention) of the polyethylene glycol-acetic acid (molecular weight 20000) of embodiment 3Y type branch

[0180] mPEG-Gly and mPEG-OCH 2 The steps of CO-NHS reaction refer to Example 2. After reacting overnight at room temperature, add BOC anhydride, react for 3 hours, concentrate the solvent by rotary evaporation, add diethyl ether to the residue, collect the precipitate by filtration, vacuum dry, purify by ion exchange chromatography, and monitor by GFC. The target product peak height exceeds 5mv to start collecting, and the collection ends when it is lower than 5mv.

[0181] The GFC chromatogram of the crude product before column separation is as follows: Figure 9 Shown, wherein the result analysis is shown in Table 9:

[0182] Table 9 Analysis result table

[0183]

[0184]

[0185] Collect the GFC chromatogram of the starting point as Figure 10 As shown, wherein the result analysis is shown in Table 10:

[0186] Table...

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Abstract

The invention discloses a preparation method for a Y-type branched hydrophilic polymer carboxylic acid derivative, and in particular relates to a preparation method for a high-purity high-molecular-weight Y-type branched polyethylene glycol carboxylic acid derivative. The method disclosed by the invention has simple preparation steps, products obtained after a reaction are easy to separate, separation costs are low, the purity and yield of the product are high, subsequent preparation of other derivatives and drug conjugates of the derivatives prepared based on preparation of the carboxylic acid derivative is facilitated, and industrial amplification and commercial applications are facilitated; and the prepared Y-type branched hydrophilic polymer carboxylic acid derivative (especially the high-molecular-weight Y-type branched polyethylene glycol carboxylic acid derivative) has high purity and high commercial value, especially has high application value in preparation of a drug for preventing and / or treating diseases.

Description

technical field [0001] The invention relates to the technical field of polymers, in particular to a method for preparing a Y-branched hydrophilic polymer carboxylic acid derivative, in particular to a high-purity, high-molecular-weight Y-branched polyethylene glycol carboxylic acid derivative. Preparation. Background technique [0002] Polyethylene glycol (PEG) is considered to be a polymer with a very low level of protein and cell absorption among known polymers, and it has good water solubility and biocompatibility, non-toxic, non-immune, and non-teratogenic It is widely used in the fields of drug modification, preparation preparation and medical device materials due to its advantages of non-antigenicity and non-antigenicity. Since 1991, after the first PEG-modified drug PEG-ADA was approved by the FDA, major pharmaceutical companies have invested a lot of energy and money in the research and development of PEG in the field of drugs. In recent years, the listed products ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00
CPCC08G81/00A61K31/00A61K47/00C08G65/3322C08G65/33396C08L2203/02C08L71/126
Inventor 陈晓萌林美娜张如军赵宣
Owner JENKEM TECH CO LTD (LIAONING)
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