2-hydroxychalcone amine compounds and application thereof
一种羟基查尔酮胺、化合物的技术,应用在一类2‑羟基查尔酮胺类化合物及其用途领域,能够解决解聚活性不理想、疗效欠佳等问题
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Embodiment 1
[0037] Example 1 General method for the preparation of 2-hydroxychalcone amines (I)
[0038] Add 2.0 mmol of the corresponding 2-hydroxyacetophenone compound (2), 3.0 mmol of the corresponding benzaldehyde compound (1) and 30 ml of ethanol into the reaction flask, stir well, then add 12.0 mmol of 30% KOH aqueous solution dropwise, Stir and react at 40-50°C for 2.0 to 72.0 hours (the reaction progress is tracked by TLC); after the reaction, cool to room temperature, adjust the pH of the reaction solution to strong acidity with 10% hydrochloric acid aqueous solution, and then adjust the pH of the reaction solution with saturated sodium bicarbonate aqueous solution To weak alkalinity, evaporate ethanol under reduced pressure, add 100 mL deionized water to the residual liquid, extract three times with 300 mL dichloromethane, combine organic layers, wash with saturated aqueous sodium chloride solution, and dry over anhydrous sodium sulfate Filtrate, evaporate the solvent under redu...
Embodiment 2
[0063] Example 2 General method for the preparation of 2-hydroxychalcone amine compound (I) and acid salt formation
[0064] Add 2.0 mmol of 2-hydroxychalcone amine compound (I) obtained according to the above Example 1 and 50 ml of acetone into the reaction flask, stir evenly, add 8.0 mmol of the corresponding acid, heat and reflux and stir for 20 minutes, and the reaction is over After cooling to room temperature, the solvent was evaporated under reduced pressure, the residue was recrystallized with acetone, and the precipitated solid was filtered to obtain the salt of 2-hydroxychalcone amine compound (I). 1 Confirmed by H NMR and ESI-MS.
Embodiment 3
[0065] Example 3 Screening results of biological activity of some 2-hydroxychalcone amine compounds (I)
[0066] .
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