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Derivatives of astilbin and preparation method thereof

A technology for astilbin and its derivatives, which is applied in the field of astilbin derivatives and their preparation, and can solve problems such as limiting clinical applications

Inactive Publication Date: 2010-02-03
SHANDONG GREENERY NATURAL MEDICINE RES & DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Astilbin has pharmacological effects such as anti-myocardial ischemia, immune regulation, anti-inflammation, and analgesia, but because it is insoluble in water, its clinical application is limited. A series of derivatives, thus expanding the clinical application

Method used

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  • Derivatives of astilbin and preparation method thereof
  • Derivatives of astilbin and preparation method thereof
  • Derivatives of astilbin and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0047] 1. Prepare the compound of the following formula:

[0048]

[0049] Dissolve astilbin in NaOH solution, pass through ethylene oxide, react at 70°C-75°C for 3 hours, let cool, add water and place overnight to obtain crude product, and obtain pure product through repeated column chromatography.

[0050] Chemical Formula: C23H26O12, Exact Mass: 494.14, Molecular Weight: 494.45, m / z: 494.14 (100.0%), 495.15 (25.6%), 496.15 (5.6%), Elemental Analysis: C, 55.87; H, 5.30; O, 38.83, Boiling Point: 1573.51[K], Melting Point: 1171.21[K], Critical Temp: 1343.6[K], Critical Press: 30.83[Bar], Critical Vol: 1193.5[cm3 / mol], Gibbs Energy: -1133.08[ kJ / mol], Log P: -0.56, MR: 118.94 [cm3 / mol], Henry's Law: 31.6, Heat of Form: -1855.66 [kJ / mol], tPSA: 245.3, CLogP: -0.0688307, CMR: 11.6666.

[0051] 2. Prepare the compound of the following formula:

[0052]

[0053] Add astilbin, DMF and anhydrous potassium carbonate into the three-necked flask, add ethyl chloroacetate dropwise...

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Abstract

The invention relates to a phenolic hydroxyl derivative, a benzene ring substituted derivative and a carbonyl derivative of astilbin, and also provides a preparation method for the derivatives.

Description

technical field [0001] The invention relates to astilbin derivatives and a preparation method thereof, in particular to astilbinol hydroxyl derivatives, benzene ring group-substituted derivatives and carbonyl-substituted derivatives. Background technique [0002] Astilbin has pharmacological effects such as anti-myocardial ischemia, immune regulation, anti-inflammation, and analgesia, but because it is insoluble in water, its clinical application is limited. A series of derivatives, thus expanding the clinical application. Contents of the invention [0003] The invention provides a phenolic hydroxyl derivative of astilbin and a preparation method thereof. [0004] The invention provides astilbin substituted derivatives with benzene ring groups and a preparation method thereof. [0005] The invention provides astilbin carboxyl-substituted derivatives and a preparation method thereof. [0006] 1. Phenolic hydroxyl derivatives: [0007] (1) Reaction with chlorohydrin or e...

Claims

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Application Information

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IPC IPC(8): C07H17/07A61P9/10A61P29/00A61P37/02
Inventor 曲桂武岳喜典
Owner SHANDONG GREENERY NATURAL MEDICINE RES & DEV
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