A kind of chalcone analog and its preparation method and use
A use and compound technology, applied in the field of compound drugs, can solve problems such as low water solubility and fat solubility, affect drug bioavailability, unfavorable clinical use, etc., achieve improved curative effect, obvious anti-tumor activity, and improved solubility problems
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Embodiment 1
[0052] Example 1 Preparation of 2,6-dihydroxy-3,4,4'-trimethoxybenzophenone
[0053] (1) Preparation of Alkyl Aglycone—5-Hydroxy-6,7,4′-Trimethoxyisoflavone
[0054] Take 500g of aglycone, add 100g of NaOH, mix well, add 1500ml of 95% ethanol to a 10-liter round bottom flask, heat and boil in a water bath for 5 minutes, then add 1000ml of dimethyl sulfate, react for 15min, take it out, and immediately wash it with hydrochloric acid Adjust the pH to acidic, add water, stir and let it cool, precipitate an off-white precipitate, filter, wash the precipitate with water until the pH of the effluent is nearly neutral, and obtain an off-white powder, recrystallize with chloroform, filter, and dry under reduced pressure at 60°C to obtain 5-hydroxyl-6, 500 g of 7,4'-trimethoxyisoflavone (white crystalline powder, the yield is 2% of the medicinal material, and the content is >98%).
[0055] After determination, the compound mp: 189~191°C (chloroform); UVλ max nm: 267, 211, 202nm (EtOH...
Embodiment 2
[0061] Example 2 Preparation of 2,6-dihydroxy-3-methoxy-4,4'-diethoxybenzophenone
[0062] (1) Preparation of Alkyl Aglycone—5-Hydroxy-6-Methoxy-7,4′-diethoxyisoflavone
[0063] Take 500g of dried aglycone, add 100g of NaOH, mix well, add 1500ml of 95% ethanol to a 10-liter round bottom flask, heat and boil in a water bath for 5 minutes, then add 1000ml of diethyl sulfate, react for 30min, take it out, and immediately wash it with hydrochloric acid Adjust the pH to acidic, add water, stir and let cool, precipitate out, filter, wash the precipitate with water until the pH of the effluent is nearly neutral, and obtain a light yellow powder, recrystallize with chloroform, filter, and dry under reduced pressure at 60°C to obtain 5-hydroxy-6- 600 g of methoxy-7,4'-diethoxy isoflavone (light yellow crystalline powder, the yield is 3% of the amount of the medicinal material, and the content is >98%).
[0064] After determination, the compound mp: 163~166°C (chloroform); UVλ max nm:...
Embodiment 3
[0071] Take 500g of dried aglycone, add 100g of NaOH, mix well, add 1000ml of iodomethane into a 10-liter round bottom flask, heat and boil in a water bath for 30 minutes, take it out, immediately adjust the pH to acidic with hydrochloric acid, add water, stir and let cool, and precipitate Off-white precipitate, filtered, washed with water until the pH of the effluent was nearly neutral, and off-white powder was obtained, which was recrystallized with chloroform, filtered, and dried under reduced pressure at 60°C to obtain 500 g of 5-hydroxy-6,7,4′-trimethoxyisoflavone (white crystalline powder, the yield is 2% of the medicinal material, and the content is >98%).
[0072] Take 100g of 5-hydroxy-6,7,4'-trimethoxyisoflavone in a round bottom flask, add 200ml of 5% NaOH aqueous solution, heat in a water bath for 2 hours, take it out, adjust the pH to acidic with hydrochloric acid, add water, stir and let cool , precipitated, filtered, washed with water until neutral to obtain a l...
PUM
Login to View More Abstract
Description
Claims
Application Information
Login to View More