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Polyphenol hydroxy flavone compound with pharmaceutical function and preparation method thereof

A compound and mixture technology, applied in the field of medicine, can solve the problems of difficult extraction and separation, scarce quantity and high cost, and achieve the effects of stable and reliable supply and quality, mature production technology and low production cost

Active Publication Date: 2012-12-26
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Only a small amount of the compound of formula I is extracted from plants through phytochemical methods. The amount is rare and only limited to the needs of small-scale experimental research. The price is extremely expensive, with a value of more than six or seven thousand yuan per gram.
Since the content of the compound of formula I in plants is very low, only a few parts per thousand, or even a few parts per ten thousand, it is difficult to extract and separate, the cost is high, it is difficult to produce in batches, and it cannot meet the actual needs

Method used

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  • Polyphenol hydroxy flavone compound with pharmaceutical function and preparation method thereof
  • Polyphenol hydroxy flavone compound with pharmaceutical function and preparation method thereof
  • Polyphenol hydroxy flavone compound with pharmaceutical function and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1 Synthesis of the compound of formula I (the catalyst used is CaCl 2 )

[0046] Take 28.0g of scutellarin raw material (equivalent to scutellarin 23.1g, 0.05mol), put it in a 1000mL round bottom flask, add 500g methanol, 0.56g CaCl 2 (0.005mol), heated and stirred at 50°C for 2h. The reaction solution was concentrated by vacuum to recover methanol. When the volume of the concentrated solution was reduced to about 1 / 3 of the original volume, the concentration was stopped, and the concentrated solution was allowed to stand and cool to room temperature. A large amount of product crystallized out. Vacuum filter, wash with 30mL cold methanol three times, try to drain, transfer the obtained product into 250mL ethyl acetate-petroleum ether (3:1), heat to boiling for 30min, put it in the refrigerator at 0-5℃ to cool for more than 4h . Take out the crystalline product, vacuum filter, wash with 30mL cold ethyl acetate three times, and finally wash with about 15mL petroleum...

Embodiment 2

[0047] Example 2 Synthesis of the compound of formula I (the catalyst used is ZnCl 2 )

[0048] Take 28.0g of scutellarin raw material (equivalent to scutellarin 23.1g, 0.05mol), put it in a 1000mL round bottom flask, add 500g methanol, 0.68g ZnCl 2 (0.005mol), heated and stirred at 50°C for 2h. The rest is the same as in Example 1 to obtain 23.3 g of the compound of formula I in a light yellow loose powder form with a yield of 97.9%.

Embodiment 3

[0049] Example 3 Synthesis of the compound of formula I (the catalyst used is MgCl 2 )

[0050] Take 28.0g of scutellarin raw material (equivalent to scutellarin 23.1g, 0.05mol), put it in a 1000mL round bottom flask, add 500g methanol, 0.48g MgCl 2 (0.005mol), heated and stirred at 50°C for 2h. The rest is the same as in Example 1 to obtain 19.3 g of the compound of formula I in a light yellow loose powder form with a yield of 81.1%.

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Abstract

The invention belongs to the field of medicines and particularly discloses a method for preparing a polyphenol hydroxy flavone compound with a pharmaceutical function. According to the invention, the method comprises the steps of: taking scutellarin and methanol as chlorides of a catalyst, and heating and reacting in a solvent to obtain the polyphenol hydroxy flavone compound. The method is moderate in reacting condition, simple in operation and high in product yield, and is convenient to realize industrialized production; and thus the method has a good industrial application prospect.

Description

Technical field [0001] The invention belongs to the field of medicine, and specifically relates to a method for preparing a polyphenol hydroxyflavonoid compound with pharmaceutical use. Background technique [0002] Human aging refers to a series of degenerative changes in morphological structure and physiological functions after the human body grows and develops to maturity with age. It is a process in which the functions of human tissues and organs decline and decline. Modern medicine believes that aging is a comprehensive manifestation of various biochemical reactions of the body. The human body produces free radicals all the time, but at the same time it has an effective free radical scavenging system (such as GSH, SOD). The two are in a balanced state, so that the free radicals in the body can be maintained at a normal level. But with age, this balance is gradually destroyed, resulting in excess free radicals. Free radicals have a strong ability to react. They can oxidize ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/07C07H1/00A61K31/7048A61P25/20A61P25/28A61P39/00
Inventor 周荣光杨兆祥
Owner KPC PHARM INC
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