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Swainsonine derivative and preparation method of research reagent of swainsonine derivative

A technology of swainsonine and derivatives, which is applied in the preparation of sugar derivatives, sugar derivatives, sugar derivatives, etc., can solve the problems of toxicity and unconnected porphyrin rings, so as to eliminate hidden dangers and produce spectacular production benefits , to avoid the effect of hepatotoxicity

Active Publication Date: 2014-11-19
毕毅良
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] At present, the problem with swainsonine is that domestic and foreign animal and clinical tests have proved that if the swainsonin solution exceeds a certain concentration, it will produce toxicity, and it must be limited to the specified concentration.
[0021] However, swainsonine is currently undergoing Phase III clinical trials abroad. Although the anti-cancer efficacy is basically positive, it is still in a difficult state of drug concentration, drug resistance and targeted drugs, and the connection of porphyrin rings has not yet been carried out.

Method used

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  • Swainsonine derivative and preparation method of research reagent of swainsonine derivative
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  • Swainsonine derivative and preparation method of research reagent of swainsonine derivative

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Embodiment Construction

[0055] The present invention will be further described below in conjunction with specific embodiments.

[0056] (1) Drugs (analytical pure) used in this example

[0057] Pure swaintonin (imported from Germany) Shanghai Haring Biotechnology Co., Ltd.

[0058] Protoporphyrin Shanghai Haling Biotechnology Co., Ltd.

[0059] Cordyceps sinensis (cordycepin) Shanghai Shifeng Biotechnology Co., Ltd.

[0060] β-Cyclodextrin Shanghai Haling Biotechnology Co., Ltd.

[0061]

[0062] The guest molecules with high solubility and organic solvents promote the separation of precipitates and inclusions.

[0063] For guest molecules that are insoluble in water, add a small amount of solvent to dissolve them and then add them to a saturated solution.

[0064] If the inclusions are precipitates, filter and wash with water, take a small amount of appropriate organic solvent to wash away the residual drug, and dry to obtain.

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Abstract

The invention provides a swainsonine derivative and a preparation method of a research reagent of the swainsonine derivative. The swainsonine is prepared through the following synthesis steps: a, adding chloroacetic acid and potassium hydroxide by taking swainsonine as a raw material and taking water as a solvent; b, feeding hematoporphyrin into thionyl chloride, and then adding cordycepin; and c, pouring the product obtained in the step a into the product obtained in the step b, and dropwise adding newly prepared potassium ethoxide into the obtained mixture, so that a swainsonine derivative solution is obtained. The swainsonine derivative disclosed by the invention is a product derived on the basis of a swainsonine structure, and by comparing, the difference is as follows: an enriched heterocyclic ring is connected, so that the swainsonine derivative disclosed by the invention has a function of enriching cancer cells, and can allow drugs to tend to parts with tumors but allow the drug concentration of other parts to be little.

Description

technical field [0001] The invention belongs to chemical synthesis technology, in particular to a swainsonine derivative. Background technique [0002] 1. The key to cancer metastasis outside the membrane is the adhesion of sialic acid [0003] Cancer is a large class of diseases characterized by abnormal cell proliferation and metastasis. More than 90% of cancer patients die from cancer metastasis. [0004] Studies have shown that cancer is a mixture of dozens or even hundreds of diseases with heterogeneous characteristics. Although cancer is quite complex, the development of cancer has a common feature: elevated sialic acid in patients. The end of the oligosaccharide chain on the surface of tumor cells is sialic acid, and the increase of the branch of sialic acid is the key link of adhesion, and it is an important reason for the shedding and adhesion of cancer cells in the process of metastasis! The present invention thinks that the behavior of cancer metastasis mainly ...

Claims

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Application Information

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IPC IPC(8): C07H19/23C07H1/00A61K31/7076A61K47/48A61P35/04
Inventor 毕毅良毕慧君
Owner 毕毅良
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