Active xanthone compound and preparation method thereof

A compound, the technology of ketone, which is applied in the field of active ketone compound and its preparation, can solve the problems of low yield and few applications

Inactive Publication Date: 2013-04-03
ZHONGBEI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] One-step synthesis method refers to the formation of ether bond and carbonyl group through one-step reaction. This method is simple and easy to operate, but this method is relatively seldom used
That is to use o-hydroxybenzoic acid and phenolic compounds as raw materials to complete the synthesis of the ketone mother nucleus in the next step under the action of polyphosphoric acid or phosphorus oxychloride, but the yield is low

Method used

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  • Active xanthone compound and preparation method thereof
  • Active xanthone compound and preparation method thereof
  • Active xanthone compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Weigh 10.913g o-aminophenol into a three-necked flask, add 100mL concentrated HCl and 100mL water, cool in an ice-salt bath, and dissolve 7gNaNO 2 and 50mL of water, move the prepared sodium nitrite solution into a constant pressure dropping funnel, slowly drop it into a three-necked bottle, stir mechanically, and control the temperature below 5°C with the dropping speed. After the dropwise addition, 0.2mol of KI solution was added dropwise under vigorous stirring, and a large amount of foam (N 2 ), heated in a water bath at 50°C after the addition, and cooled. Then extract with an appropriate amount of ether, using Na 2 S 2 o 3 Solution washing, washing with water, with anhydrous MgSO 4 After drying, one-step intermediate o-iodophenol is obtained.

[0033] Add 100ml of toluene into the three-necked flask as a solvent, then add 22.03g of the one-step intermediate and 25.2g of phloroglucinol, and add the dehydrating agent POCl into the three-necked flask equipped wi...

Embodiment 2

[0037] Antibacterial activity experiments were carried out on the target compound 2,4-dihydroxykoushanone. Gram-positive bacteria Staphylococcus aureus and Gram-negative bacteria Escherichia coli were selected as indicator bacteria, and gentamicin sulfate was used as reference sample. Experiments show that: 2,4-dihydroxykoushanone has a certain antibacterial effect on Escherichia coli, and has a very good antibacterial effect on Staphylococcus aureus.

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PUM

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Abstract

The invention discloses an active xanthone compound, which has a structure represented by a general formula (I) as follows. 2,4-dihydroxyl xanthones differing in concentration represent different degrees of antibacterial effects on staphylococcus aureus, therefore the active xanthone compound has a remarkable inhibiting effect.

Description

technical field [0001] The invention relates to the field of pharmaceutical compounds, in particular to an active ketone compound with antibacterial effect and a preparation method thereof. Background technique [0002] Koshanone is also called dibenzo-γ-pyrone, xanthone, xanthone, etc. It is a substance that has a stronger antioxidant effect than vitamin C and vitamin E. It has heat-clearing, detoxifying, anti-inflammatory, Liver protection, choleretic, diuretic, antibacterial, anticancer, antimalarial, antidepressant, antioxidative and other physiological activities, its derivatives are widely distributed in nature, and are one of the active ingredients of medicinal plants, with high medicinal value . Scutellaria baicalensis of the family Gentianaceae, which is rich in ketones, is a common folk medicine of the Naxi, Tibetan, and Miao nationalities. Polygala urophylla mainly distributed in southwest my country is rich in ketones, and its roots are used as medicine in the f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/86A61P31/04
Inventor 马雪梅郑志花李志春潘婕李红鹏
Owner ZHONGBEI UNIV
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