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Magnetic water-soluble fullerene, and preparation method and application thereof

A fullerene, water-soluble technology, applied in the field of medicine, can solve the problems of poor targeting, weak water-solubility of fullerene, low biocompatibility, etc., and achieves low cost, good physical and chemical stability, and water dispersion. strong effect

Inactive Publication Date: 2013-08-07
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In view of the above situation, in order to solve the defects of the prior art, the object of the present invention is to provide a kind of magnetic water-soluble fullerene and its preparation method and application, which can effectively solve the problem of weak water solubility and low biocompatibility of existing fullerene. , the problem of poor targeting

Method used

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Examples

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preparation example Construction

[0013] The preparation method of described magnetic water-soluble fullerene is realized by the following steps:

[0014] 1) Dissolve 100 mg of fullerene in 100 ml of toluene, add 0.5 g of sodium hydride, stir evenly, add 0.3 ml of diethyl bromomalonate, protect with nitrogen, stir at room temperature 15-25°C for 5 hours, filter to remove sodium hydride, Toluene was removed by rotary evaporation, and vacuum-dried at 60°C for 24 hours to obtain a fullerene substituted with diethyl bromomalonate;

[0015] 2) Add 1 g of the above-mentioned fullerene substituted by diethyl bromomalonate and sodium hydride into 50 ml of toluene, hydrolyze at 80 ° C until the toluene phase is colorless, pour off the toluene, add 20 ml of concentrated hydrochloric acid, filter to obtain a filter cake, and take The filter cake was dissolved in 100ml of methanol, filtered to remove insoluble matter, methanol was removed by rotary evaporation, and vacuum-dried at 60°C for 24 hours to obtain malonate-subs...

Embodiment 1

[0043] 1) Dissolve 100 mg of fullerene in 100 ml of toluene, add 0.5 g of sodium hydride, stir evenly, add 0.3 ml of diethyl bromomalonate, protect with nitrogen, stir at room temperature 15-25°C for 5 hours, filter to remove sodium hydride, Toluene was removed by rotary evaporation, and vacuum-dried at 60°C for 24 hours to obtain a fullerene substituted with diethyl bromomalonate;

[0044] 2) Add 1 g of the above-mentioned fullerene substituted by diethyl bromomalonate and sodium hydride into 50 ml of toluene, hydrolyze at 80 ° C until the toluene phase is colorless, pour off the toluene, add 20 ml of concentrated hydrochloric acid, filter to obtain a filter cake, and take The filter cake was dissolved in 100ml of methanol, filtered to remove insoluble matter, methanol was removed by rotary evaporation, and vacuum-dried at 60°C for 24 hours to obtain malonate-substituted fullerene (C 60 -COOH) 84mg.

[0045] 3) Fully dissolve 50 mg of the above malonic acid-substituted fulle...

Embodiment 2

[0048] 1) Dissolve 100 mg of fullerene in 100 ml of toluene, add 0.5 g of sodium hydride, stir evenly, add 0.3 ml of diethyl bromomalonate, protect with nitrogen, stir at room temperature 15-25°C for 5 hours, filter to remove sodium hydride, Toluene was removed by rotary evaporation, and vacuum-dried at 60°C for 24 hours to obtain a fullerene substituted with diethyl bromomalonate;

[0049] 2) Add 1 g of the above-mentioned fullerene substituted by diethyl bromomalonate and sodium hydride into 50 ml of toluene, hydrolyze at 80 ° C until the toluene phase is colorless, pour off the toluene, add 20 ml of concentrated hydrochloric acid, filter to obtain a filter cake, and take The filter cake was dissolved in 100ml of methanol, filtered to remove insoluble matter, methanol was removed by rotary evaporation, and vacuum-dried at 60°C for 24 hours to obtain malonate-substituted fullerene (C 60 -COOH) 86mg.

[0050] 3) Fully dissolve 50 mg of the above malonic acid-substituted fulle...

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Abstract

The invention relates to a magnetic water-soluble fullerene, and a preparation method and application thereof. The invention effectively solves the problems of low water solubility, low compatibility and poor targeting property of the fullerene. The method comprises the following steps: dissolving fullerene in toluene, adding sodium hydride and diethyl bromomalonate, stirring in a nitrogen protective atmosphere to remove sodium hydride and toluene, adding the dried diethyl-bromomalonate-substituted fullerene into the toluene, hydrolyzing until the toluene phase becomes colorless, adding concentrated hydrochloric acid, filtering to obtain a filter cake, removing insoluble substances and methanol, drying to obtain malonic-acid-substituted fullerene, dissolving in an ethylene glycol and di-acetal mixed solvent, adding sodium acetate and ferric iron salt to react, washing, drying to obtain ferroferric-oxide-carried fullerene, carrying out ultrasonic dispersion on the ferroferric-oxide-carried fullerene, amino water-soluble substance and EDC.HCl in phosphate, reacting in a dark place, carrying out vacuum filtration, and drying to obtain the magnetic water-soluble fullerene. The magnetic water-soluble fullerene has the advantages of favorable magnetic targeting propertt, strong water dispersity, low toxicity for organisms, high physical and chemical stability, good quality and low cost.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a magnetic water-soluble fullerene and its preparation method and application. Background technique [0002] The discovery of the fullerene family, the third allotrope of carbon, is one of the most important breakthroughs in the history of natural science in the last century. Kroto and others also won the 1996 Nobel Prize in Chemistry for their pioneering work in the study of fullerenes. Fullerene has attracted much attention due to its unique structure and properties. In the past ten years, scientists from almost all famous universities and research institutes in the world have carried out research related to fullerene. It has become a common concern of researchers in physics, chemistry, materials and life sciences. The important scientific significance of fullerene molecules was named "Star Molecule" in 1991 by the American "Science" magazine. Among nanomaterials, carbon nanomaterial...

Claims

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Application Information

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IPC IPC(8): A61K49/06A61K41/00A61K47/32A61K47/34A61K47/02A61K47/04A61P35/00
Inventor 史进进余晓媛王蕾张静张振中马柔柔刘艳刘瑞瑗高君潘晶晶
Owner ZHENGZHOU UNIV
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