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Tripterygium wilfordii derivative and application

A technology of Tripterygium wilfordii and its derivatives, applied in the field of tripterygium wilfordii derivatives and applications, can solve the problems of limiting the large-scale application of tripterygium wilfordii, high toxicity and side effects of tripterygium wilfordii, poor physical and chemical properties, etc., achieve low cost, increase application performance, The effect of improving physical and chemical properties

Inactive Publication Date: 2019-06-18
SHANGHAI UNIV OF MEDICINE & HEALTH SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, long-term clinical application practice has found that Tripterygium wilfordii has high toxic and side effects, such as gastrointestinal tract, reproductive system, blood system and other side effects are particularly obvious, plus the poor physical and chemical properties of tripterygium, all limit the use of tripterygium wilfordii in Clinical large-scale application

Method used

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  • Tripterygium wilfordii derivative and application
  • Tripterygium wilfordii derivative and application
  • Tripterygium wilfordii derivative and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Preparation;

[0041] Step 1: Dissolve 3-hydroxybenzoic acid (3g), dimethylamine tetrahydrofuran solution (10mL) and HATU (5g) in dichloromethane (10mL), and stir overnight at room temperature. After the reaction, extract with dichloromethane, the organic phase was washed with dilute hydrochloric acid and distilled water, dried, and concentrated under reduced pressure to obtain the compound 3-hydroxy-N,N-dimethylbenzamide (2.1g, white solid), which was used directly In the next step reaction.

[0042] Step 2: Dissolve 3-hydroxy-N,N-dimethylbenzamide (2g) and 3-fluoro-4-nitrobenzaldehyde (2.5g) in anhydrous DMF (15mL) under nitrogen protection Add anhydrous potassium carbonate powder (4g). React at 80°C for 3h, cool to room temperature, extract with dichloromethane, dry the organic phase, concentrate, crystallize with methyl tert-butyl ether to obtain compound 3-(5-aldehyde-2-nitrophenoxy)-N,N -Dimethylbenzamide (1.8 g, white solid).

[0043] Step 3: Add 3-(5-aldehyde-2-ni...

Embodiment 2

[0047] Using the same method as in the first and second steps of Example 1, and replacing the anhydrous ethanol in the third part with anhydrous methanol, which is:

[0048]

[0049] Then react with triptolide to produce

Embodiment 3

[0051] Using the same method as in Example 1, 3-(5-(hydroxyethyl)-2-nitrophenoxy)-N,N-dimethylbenzamide was prepared,

[0052] Then react with triptolide to produce

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Abstract

The invention relates to a tripterygium wilfordii derivative, preparation and application thereof. The tripterygium wilfordii derivative has a molecular formula shown as the specification. Compared with the prior art, the tripterygium wilfordii derivative provided by the invention can effectively reduce the toxic and side effects of tripterygium wilfordii extract and enhance the physical and chemical properties, and increases the application performance of tripterygium wilfordii; the tripterygium wilfordii derivative is simple in synthesis and low in cost; and the tripterygium wilfordii derivative can be applied to preparation of drugs treating or preventing tumors or inflammatory-immune diseases, and has wide application.

Description

Technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a derivative of Tripterygium wilfordii and its application. Background technique [0002] Tripterygium wilfordii (scientific name: Tripterygium wilfordii) is a woody vine plant of the genus Tripterygium of the Eucalyptus family. It is mainly produced in Yunnan, Zhejiang, Fujian and other places. It is used as medicine with roots, leaves, flowers and fruits. Triptolide, also known as Triptolide, is an epoxidized diterpene lactone compound isolated from Tripterygium wilfordii. It is the main active component of Tripterygium wilfordii. It has the functions of detoxification and dispelling, promoting blood circulation and removing blood stasis, and strengthening the body. In recent years, it has been found that triptolide has shown strong anti-tumor activity and broad-spectrum anti-tumor activity in in vivo and in vitro model studies of various malignant tumors, including anti-evil, ant...

Claims

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Application Information

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IPC IPC(8): C07J73/00C07J63/00A61K31/585A61K31/58A61K31/56A61P35/00A61P35/02A61P19/04A61P19/02A61P29/00A61P37/02A61P25/00A61P1/00A61P5/14A61P17/00
Inventor 周兆丽黄钢王慧
Owner SHANGHAI UNIV OF MEDICINE & HEALTH SCI
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