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Dobby polyethylene glycol and its active derivative

A multi-arm polyethylene glycol and derivative technology, which is applied in the directions of organic active ingredients, medical preparations of non-active ingredients, organic chemistry, etc., can solve the problem of narrow molecular weight distribution, insufficient purity of multi-arm polyethylene glycol, and molecular weight distribution. leniency issues

Inactive Publication Date: 2017-09-26
JENKEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, U.S. Patent 6858736 describes a six-arm polyethylene glycol with sorbitol as the central molecular initiator, but for the requirement of more than six arms, sugar molecules have limitations as the central molecular initiator
[0008] The purpose of the present invention is to overcome the defects of insufficient purity and wide molecular weight distribution of multi-armed polyethylene glycol in the prior art, and provide a multi-armed polyethylene glycol with novel structure, narrow molecular weight distribution and high purity and its preparation method, and the obtained The multi-arm polyethylene glycol active derivative, the formed gel and its combination with drug molecules and applications

Method used

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  • Dobby polyethylene glycol and its active derivative
  • Dobby polyethylene glycol and its active derivative
  • Dobby polyethylene glycol and its active derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0211] Embodiment 1: synthetic glycerol triglyceride

[0212] Synthesize glycerol triglyceride ether of following structure:

[0213]

[0214] Add glycerol (0.1mol), dimethyl sulfoxide (100mL) and potassium hydroxide (0.6mol) in the there-necked flask, stir in a water bath, then drop epichlorohydrin (0.9mol) in the reaction system, control The reaction temperature did not exceed 35°C, and the reaction was carried out overnight at room temperature. After the reaction, the reaction solution was filtered, and the filter residue was washed with dichloromethane, then the filtrate was collected, and the dichloromethane was removed by rotary evaporation, and finally washed with saturated brine, extracted with ethyl acetate, and rotary evaporated to obtain a crude product. The crude product was molecularly distilled to obtain pure glycerol glycidyl ether.

[0215] The obtained glycerol glycidyl ether (1 g) was dissolved in 10 mL of purified water, and then potassium hydroxide was...

Embodiment 2

[0219] Embodiment 2: Synthesis of Tetraglycerol Tetraglycerol Ether

[0220] Synthesize tetraglycerol tetraglyceride of following structure:

[0221]

[0222] Add tetramethylene glycol (0.1mol), dimethyl sulfoxide (100mL) and potassium hydroxide (0.8mol) in the there-necked flask, stir in a water bath, then drip epichlorohydrin (1.2mol) in the reaction system, control The reaction temperature did not exceed 35°C, and the reaction was carried out overnight at room temperature. After the reaction, the reaction solution was filtered, and the filter residue was washed with dichloromethane, then the filtrate was collected, and the dichloromethane was removed by rotary evaporation, and finally washed with saturated brine, extracted with ethyl acetate, and rotary evaporated to obtain a crude product. The crude product was molecularly distilled to obtain pure butanetrol glycidyl ether.

[0223] The obtained tetramethylene glycol glycidyl ether (1 g) was dissolved in 10 mL of puri...

Embodiment 3

[0227] Embodiment 3: Synthesis of Pentapentyl Pentaglyceryl Ether

[0228] Synthesize Pentapentyl Pentaglyceryl Ether of the following structure:

[0229]

[0230] Add pentapentyl alcohol (0.1mol), dimethyl sulfoxide (100mL) and potassium hydroxide (1.0mol) in the there-necked flask, stir in a water bath, then drop epichlorohydrin (1.5mol) in the reaction system, control The reaction temperature did not exceed 35°C, and the reaction was carried out overnight at room temperature. After the reaction, the reaction solution was filtered, and the filter residue was washed with dichloromethane, then the filtrate was collected, and the dichloromethane was removed by rotary evaporation, and finally washed with saturated brine, extracted with ethyl acetate, and rotary evaporated to obtain a crude product. The crude product was molecularly distilled to obtain pure pentapentyl glycidyl ether.

[0231] The obtained pentapentyl glycidyl ether (1 g) was dissolved in 10 mL of purified w...

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Abstract

The invention belongs to the technical field of a macromolecular function material, and particularly relates to a novel narrow-distributed / high-purity dobby polyethylene glycol formed by using polyhydric alcohol glyceryl ether as initiator to polymerize ethylene oxide, and its active derivative. The dobby polyethylene glycol has a structure of a general formula II, wherein B is polyhydric alcohol group and n is integer from 3 to 22; PEG is the same or different -(OCH2CH2)m-, the mean value of m is integer ranged from 3 to 250; number-average molecular weight of the dobby polyethylene glycol is 1500-80000. The invention further provides gel formed by active derivative of the narrow-distributed / high-purity dobby polyethylene glycol, a drug composition formed by the gel and the drug molecule and its application in drug preparation.

Description

technical field [0001] The invention belongs to the technical field of polymer functional materials, and in particular relates to a multi-arm polyethylene glycol with polyol glycerol ether as the core and its active functional group derivatives, drug conjugates, gel materials and preparation methods thereof, and its Application in drug carrier and medical device gel. Background technique [0002] Polyethylene glycol and its derivatives are widely used in biomedicine, pesticides, and medical materials due to their unique properties. Polyethylene glycol has a clear metabolic process in the human body, and is a safe synthetic polymer material without side effects. For example, after protein, polypeptide or drug is combined with polyethylene glycol, it can effectively prolong the physiological half-life of the combined drug and reduce the immunogenicity and toxicity of the drug. In clinical use, polyethylene glycol and its derivatives have been used in many commercial drugs as...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/28C07C41/03C07C43/13A61K47/60A61K47/69A61K9/06A61K31/4745
CPCA61K31/4745C07C41/03C08G65/2609C07C43/13A61K31/337A61K31/4741A61K47/60C08G65/327C08G65/3312C08G65/3322C08G65/33337C08G65/34C08G2650/32C08G2650/38C08G2650/50C07C43/135C08G65/33317C08G65/3344
Inventor 魏真林美娜朱振刚赵宣
Owner JENKEM TECH
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