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Novel 10-hydroxy camptothecin site-20 derivative preparation method, and application of 10-hydroxy camptothecin site 20 derivative in anti-tumor drugs

A technology of hydroxycamptothecin and derivatives, applied in the field of new compound preparation, can solve the problems of low antitumor activity and high toxicity

Inactive Publication Date: 2014-06-18
TIANJIN UNIVERSITY OF SCIENCE AND TECHNOLOGY
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, 10-hydroxycamptothecin for clinical use is an unmodified natural product with high toxicity and low antitumor activity, so its clinical application is limited.

Method used

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  • Novel 10-hydroxy camptothecin site-20 derivative preparation method, and application of 10-hydroxy camptothecin site 20 derivative in anti-tumor drugs
  • Novel 10-hydroxy camptothecin site-20 derivative preparation method, and application of 10-hydroxy camptothecin site 20 derivative in anti-tumor drugs
  • Novel 10-hydroxy camptothecin site-20 derivative preparation method, and application of 10-hydroxy camptothecin site 20 derivative in anti-tumor drugs

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Experimental program
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Effect test

Embodiment Construction

[0039] synthetic route

[0040]

[0041] Description 1

[0042] 10-tert-butoxycarbonyl-camptothecin

[0043] 10-Hydroxycamptothecin (1g, 2.74mmol) was added to a 100mL round-bottomed flask, then DMF (28mL) was added to dissolve, and then di-tert-butyl dicarbonate (1.2g, 5.5mmol) was added after fully dissolved, and stirred After 5 minutes, pyridine (10 mL) was added, the bottle was plugged, and the reaction was placed in a dark place for 24 hours. After the reaction is over, pour the reaction solution into a 250mL separatory funnel, add 90mL of dichloromethane to dissolve, then add 150mL of water each time for extraction, and extract three times; then add 36mL of 1mol / L hydrochloric acid and 114mL of water for extraction, and extract three times in the same way ; Finally, extract it once with 150mL saturated saline. Anhydrous NaSO for organic phase 4 Dry, spin off the solvent under reduced pressure, dichloromethane:methanol=120:1, 200-300 mesh silica gel column purific...

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Abstract

The present invention relates to a novel 10-hydroxy camptothecin site-20 derivative preparation method, and an application of the 10-hydroxy camptothecin site-20 derivative in anti-tumor drugs. According to the present invention, 10-hydroxy camptothecin is adopted as a raw material, and hydroxy protection, condensation reaction, substitution reaction, deprotection and other reactions are performed to obtain the derivative with characteristics of anticancer activity and increased 10-hydroxy camptothecin water-solubility.

Description

technical field [0001] The invention belongs to the field of preparation methods of new compounds, in particular a novel preparation method of 20-position derivatives of 10-hydroxycamptothecin and its application in antitumor drugs. Background technique [0002] According to the estimates of the World Health Organization, about 5 million people in the world die from various malignant tumors every year, and only 1.3 million cases of cancer are diagnosed in the United States every year. Cancer has become one of the diseases that seriously endanger human life and health and are difficult to cure. Camptothecin (CPT) is an anticancer drug derived from plants, which is extracted from camptothecin distributed in south-central and southwest China. Early biological experiments showed that natural camptothecin has obvious anti-tumor activity, especially for digestive tract, leukemia, and bladder cancer. [0003] Camptothecin and its derivatives are potent topoisomerase I inhibitors....

Claims

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Application Information

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IPC IPC(8): C07D491/22A61K31/4745A61P35/00A61P35/02
CPCC07D491/22
Inventor 郁彭温少鹏贾海永郭娜吕建吕蕾王义乾宋彬彬
Owner TIANJIN UNIVERSITY OF SCIENCE AND TECHNOLOGY
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