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Artemisinin derivatives and application thereof

A derivative, halogen technology, applied in the field of medicine

Inactive Publication Date: 2011-04-13
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Recent clinical studies have shown that molecular targeted therapy drugs are prone to drug resistance in vivo and traditional cytotoxic drugs have severe side effects

Method used

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  • Artemisinin derivatives and application thereof
  • Artemisinin derivatives and application thereof
  • Artemisinin derivatives and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0119] Add dihydroartemisinin (200 mmol, 56.8 g) and sodium azide 39 g (600 mmol) into (800 mL) dichloromethane solution, cool to 0-5°C after addition, and add in batches Chlorotrimethylsilane (300 mmol, 38.1 mL), and then add a catalytic amount of sodium iodide, rise to room temperature and react for 28 hours. After the reaction is complete, pour the reaction solution into 800 mL of water, extract with dichloromethane, and combine the extracted liquid, washed with water, and dried over anhydrous sodium sulfate. Evaporated to dryness to obtain oil, separated by column chromatography to obtain optically pure 10 α -Azidodihydroartemisinin 3.0 g and 10 β - Azidodihydroartemisinin 29.0 g, the yields were 5% and 47%, respectively, MS: 332.2 (M+ Na).

[0120] Step B: 10 α- Preparation of Aminodihydroartemisinin

[0121] will be 10 α - Azidodihydroartemisinin 3.0 g (9.7 mmol) was gradually added to the tetrahydrofuran solution, and at room temperature, 5.1 g (19.4 mmol) of triph...

Embodiment 2

[0132] Example 3:

[0133] (10 S )- N -{4-[3-(4-Methylsulfonylphenyl)-2-( E )-acryloyl]phenoxyacetyl}aminodihydroartemisinin

Embodiment 3

[0135] Example 4:

[0136] (10 S )- N -{4-[3-(4-Trifluoromethoxyphenyl)-2-( E )-acryloyl]phenoxyacetyl}aminodihydroartemisinin

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Abstract

The invention relates to artemisinin derivatives shown as a general formula I, and optical isomers and pharmaceutically acceptable salts thereof, wherein substituents Z, Ar, R and n are defined in the specification. The invention also relates to application of the compounds with the general formula I in preparing medicaments for treating and / or preventing cancers.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to new artemisinin derivatives, their optically active bodies and their pharmaceutically acceptable salts, including their preparation methods and pharmaceutical compositions containing the compounds. The present invention also relates to the use of the derivative in the preparation of medicines for treating and / or preventing cancer. Background technique [0002] Cancer is a disease that seriously threatens human life. According to the statistics of WHO in 2008, the number of cancer deaths in 2007 reached 7.9 million, accounting for about 13% of all deaths. In recent years, with the deepening of the research on the mechanism of tumorigenesis, the molecular mechanism of the occurrence and development of cancer has been continuously revealed, and anti-tumor drugs have developed from the initial cytotoxic drugs to the research on drugs that act on tumor-specific targets. Recent clinica...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/20A61K31/357A61K31/381A61K31/4433A61K31/36A61P35/00A61P35/02
Inventor 宫平翟鑫赵燕芳刘亚婧
Owner SHENYANG PHARMA UNIVERSITY
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