Four kinds of tripterygium wilfordii derivative and preparing method of pharmaceutics thereof

A technology of triptolide and its derivatives, which can be applied in the direction of anti-inflammatory agents, drug combinations, and pharmaceutical formulations, and can solve problems such as hindering research and development, and large toxic and side effects

Inactive Publication Date: 2008-08-06
北京美迪克斯生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Due to the pharmacological activity of triptolide, it is very likely to become a promising new drug for cl

Method used

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  • Four kinds of tripterygium wilfordii derivative and preparing method of pharmaceutics thereof
  • Four kinds of tripterygium wilfordii derivative and preparing method of pharmaceutics thereof
  • Four kinds of tripterygium wilfordii derivative and preparing method of pharmaceutics thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Synthesis of 2-(1-piperidinyl) triptolide acetate

[0032] Put 1 gram of triptolide and 1.70 grams of dimethylaminopyridine in a 100-ml round-bottomed flask, add 35 ml of dichloromethane to dissolve, and add 0.78 ml of chloroacetyl chloride dropwise in an ice-water bath. Stir overnight at room temperature, and monitor the completion of the reaction by thin-layer chromatography on a silica gel plate, add 20 ml of 0.5 equivalent hydrogen chloride solution for washing, and then add ice water for washing. Collect the dichloromethane solution, add anhydrous sodium sulfate for dehydration, filter, and concentrate at room temperature to obtain 1.26 g of solid.

[0033] 1.26 g of the solid was dissolved in dichloromethane, separated and purified with a silica gel column, eluted with a mobile phase of cyclohexane:ethyl acetate (1:1), detected by thin-layer chromatography on a silica gel G plate, and the color-developed part was collected. It was concentrated under reduced press...

Embodiment 2

[0037] Preparation of triptolide hydrochloride 2-dimethylaminoacetate

[0038] Put 1 gram of triptolide and 1.70 grams of dimethylaminopyridine in a 100-ml round-bottomed flask, add 35 ml of dichloromethane to dissolve, and add 0.78 ml of chloroacetyl chloride dropwise in an ice-water bath. Stir overnight at room temperature, and monitor the completion of the reaction by thin-layer chromatography on a silica gel G plate, add 20 ml of 0.5 equivalent hydrogen chloride solution for washing, and then add ice water for washing. Collect the dichloromethane solution, add anhydrous sodium sulfate for dehydration, filter, and concentrate at room temperature to obtain 1.61 g of solid.

[0039] 1.26 g of the solid was dissolved in dichloromethane, separated and purified with a silica gel column, eluted with a mobile phase of cyclohexane:ethyl acetate (1:1), detected by thin-layer chromatography on a silica gel G plate, and collected the colored part. Concentrate under reduced pressure a...

Embodiment 3

[0044] Preparation of 2-Dimethylaminoacetate Triptolide Hydrochloride Lyophilized Powder for Injection

[0045] Weigh 1 g of 2-dimethylaminoacetate triptolide hydrochloride, 4.5 g of sodium chloride, add distilled water to 500 ml, stir to dissolve, filter with a 0.22 micron membrane filter, and pack into 5 ml vials. 1 ml per vial, lyophilized. Get 500 bottles of freeze-dried powder injections containing 2 mg of triptolide hydrochloride per bottle.

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PUM

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Abstract

The invention provides four triptolide derivatives and a preparation method of corresponding agents, which uses triptolide as raw material, via acylation and nucleophilic substitution to obtain triptolide derivative to be reacted with acid or alkyl halide to obtain a corresponding salt which can be added with one or more pharmaceutically acceptable adjuvants to prepare relative agent-freeze-driedpowder.

Description

technical field [0001] The invention relates to a preparation method of four triptolide derivatives and preparations thereof. Background technique [0002] Triptolide, also known as triptolide or triptolide, is a diterpene lactone compound isolated from Tripterygium wilfordii or the same plant as Kunming Begonia. A large number of experimental studies at home and abroad have shown that triptolide has various pharmacological activities, and its pharmacological effects are extremely strong. For example, it has good anti-inflammatory effect and cartilage protection effect on rheumatoid arthritis [Chen Shaofang et al. Anti-inflammatory effect of triptolide [J]. Chinese herbal medicine. 1988: 19 (8): 24] [Zheng Younan et al. Triptolide Anti-inflammatory effect of ester [J]. Chinese Pharmacological Journal. 1994: 15 (6): 540], strong immunosuppressive effect [Yu Yu, Zeng Yaoying, Liu Liang, etc. Triptolide activates mouse lymphocytes in vitro The inhibitory effect of triptolide ...

Claims

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Application Information

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IPC IPC(8): C07D493/22A61K31/365A61K9/19A61P29/00A61P19/02
Inventor 贺卫国王莉安锦华
Owner 北京美迪克斯生物技术有限公司
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