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Preparation method of Schiff base two-dimensional polymer drug carrier material

A technology of carrier materials and polymers, which is applied in drug combinations, antineoplastic drugs, organic chemistry, etc., can solve the problem of low bioavailability of 5-fluorouracil, and achieve the effect of increasing bioavailability, low production cost, and mild conditions

Inactive Publication Date: 2017-02-22
HARBIN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to solve the problem that the existing 5-fluorouracil bioavailability is not high, and provide a kind of preparation method of Schiff base two-dimensional polymer drug carrier material

Method used

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  • Preparation method of Schiff base two-dimensional polymer drug carrier material
  • Preparation method of Schiff base two-dimensional polymer drug carrier material
  • Preparation method of Schiff base two-dimensional polymer drug carrier material

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specific Embodiment approach 1

[0024] Specific embodiment one: the preparation method of a kind of Schiff base two-dimensional polymer drug carrier material of the present embodiment is carried out according to the following steps:

[0025] 1. Preparation of the precursor trihydrazine triazine: disperse cyanuric chloride in absolute ethanol, then add hydrazine hydrate aqueous solution at a rate of 5mL / min to 7mL / min, heat to a temperature of 40-60°C, and place React in a constant temperature water bath at a temperature of 40-60°C for 1.5h-2.5h, then wash and filter with suction to obtain the precursor trihydrazinetriazine;

[0026] The ratio of the quality of cyanuric chloride described in step 1 to the volume of dehydrated alcohol is 9.24g: (20~40) mL;

[0027] The mol ratio of cyanuric chloride and hydrazine hydrate in the hydrazine hydrate aqueous solution described in step 1 is 0.05:(0.4~0.5);

[0028] 2. Preparation of Schiff base two-dimensional polymer drug carrier material: trimethylbenzene, 1,4-di...

specific Embodiment approach 2

[0033] Specific embodiment two: the difference between this embodiment and specific embodiment one is: the ratio of the quality of cyanuric chloride described in step one to the volume of absolute ethanol is 9.24g:30mL. Other steps and parameters are the same as those in the first embodiment.

specific Embodiment approach 3

[0034] Specific embodiment three: the difference between this embodiment and specific embodiment one or two is: the molar ratio of cyanuric chloride and hydrazine hydrate in the hydrazine hydrate aqueous solution described in step one is 0.05:0.45. Other steps and parameters are the same as those in Embodiment 1 or 2.

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Abstract

The invention relates to a preparation method of a Schiff base two-dimensional polymer drug carrier material. The invention aims at solving the problem that the existing 5-fluorouracil is lower in bioavailability. The method comprises the steps of 1, preparing a precursor-trihydrazine triazine; 2, preparing the Schiff base two-dimensional polymer drug carrier material. The Schiff base two-dimensional polymer drug carrier material can improve the bioavailability of the 5-fluorouracil and an anti-tumor treatment effect. The preparation method of the Schiff base two-dimensional polymer drug carrier material is simple and controllable in preparation technology, mild in conditions and simple in raw materials, thus being low in production cost and suitable for industrial production.

Description

technical field [0001] The invention relates to a preparation method of a Schiff base two-dimensional polymer drug carrier material. Background technique [0002] 5-Fluorouracil (5-Fu) is an anti-tumor drug commonly used clinically at present. It can inhibit the spread of thymine nucleotide synthetase to block the conversion of deoxypyrimidine nucleotides into thymine nucleotides, thereby interfering with DNA synthesis. synthesis. However, due to its obvious metabolism, short half-life, low lipophilicity and other shortcomings, the bioavailability of 5-fluorouracil is low, which greatly affects the anti-tumor efficacy. In order to reduce its toxic and side effects, a lipophilic group can be introduced into the 5-Fu molecule, and some of the prepared drugs have been used clinically, such as Tegafur (Tegfur) and 1-hexylcarbamoyl-5-fluorouracil HCFU. People have done a lot of chemical modification of 5-Fu with small molecule amino acids, glucose, short peptides and glyceropho...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D251/66C08G12/30A61K31/513A61K47/18A61K47/34A61P35/00
CPCC07D251/66A61K31/513A61K47/18A61K47/34C08G12/30
Inventor 张凤鸣赵耀张璐璐高广阔康鑫于浩
Owner HARBIN UNIV OF SCI & TECH
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