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Polyasparagine derivative containing high-activity hydrosy radical

A technology for polyasparagine and derivatives, which is applied in the field of polyasparagine derivatives, can solve the problems of unfavorable polar medicinal chemical bonding, unfavorable chemically bound medicines, small number of active hydroxyl groups, etc., and achieves that the preparation method is simple and feasible, Widespread application prospects and the effect of large drug loading

Inactive Publication Date: 2004-08-04
SURFACE & INTERFACE CHEM ENG TECH RES CENT NANJING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

As the chain length of the non-polar substituent increases, the lipophilicity of these polyasparagine derivatives gradually increases, but their hydrophilicity decreases, which is not conducive to the chemical bonding of polar drugs.
[0007] To sum up, at present, various polyasparagine derivatives generally have the problem that the number of active hydroxyl groups on the side chain is relatively small, which is not conducive to chemically bonding drugs.

Method used

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  • Polyasparagine derivative containing high-activity hydrosy radical
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Embodiment Construction

[0017] The present invention will be described in further detail below in conjunction with the accompanying drawings.

[0018] According to the present invention, a polyasparagine derivative rich in active hydroxyl groups is prepared. Its preparation method is as follows: firstly weigh 200 grams of aspartic acid, add 10 grams of catalyst concentrated phosphoric acid, and carry out polycondensation reaction at 180 ° C. React for 10 hours, gradually reduce the pressure to 1×10 4 Pa, polysuccinimide (code name: PSI) can be obtained with a yield of 95%; then 50 grams of PSI are dissolved in 250ml N,N-dimethylformamide (code name: DMF), cooled to 0°C At this temperature, 120 milliliters of diethanolamine was added dropwise, reacted at room temperature for 4 hours, the mixture was added dropwise to 1500 milliliters of n-butanol and stirred continuously, filtered after standing for 1 hour, washed with acetone until the pH value of the filtrate was neutral , vacuum-dried at room temp...

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Abstract

A polyasparagine derivative containing high-activity hydroxy radicals for medical purpose is disclosed, which features high power of carrying chemical medicine.

Description

1. Technical field: [0001] The invention relates to a medical polyamino acid polymer compound, in particular to a polyasparagine derivative rich in active hydroxyl groups. 2. Background technology: [0002] Polyamino acids and their derivatives are a new type of medical polymer compounds with excellent biocompatibility, can be completely degraded and absorbed when acting on organisms, and are non-toxic and have no side effects. [0003] At present, American Signam company has already listed poly(α,β-N-hydroxyethyl-DL-aspartamide) [Poly-(hydroxyethyl-DL-aspartamide, code name: PHEA), its main application is prodrug carrier and Plasma substitute, the structural formula is: [0004] [0005] Due to the structure of the side chain -NH-CH 2 -CH 2 OH is used as a carrier, so the number of hydroxyl groups is relatively small, which is not conducive to chemically bonding drugs, and the cost of preparation is high, and the sales price of finished products is expensive, above 10...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G69/08
Inventor 沈健陈强
Owner SURFACE & INTERFACE CHEM ENG TECH RES CENT NANJING UNIV
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