Synthesis And Structure Design Of Flavonol Derivatives

People diet all kinds of substances including flavones per day, which are widely distributed throught the plant medicament and have less side-effect and extensive pharmacology effect. Flavonols' water solubility is not better because of plane structure and crowed formation, which limit their pharmacology effect and absorption pass, as quercetin and kaempferol are the samples. It will be the further direction, when the medicine matrix isn't changed. It is easier to link to other radicels because of flavonols' A and B ring. It's impossible to synthesize their derivatives by chemical way, with the development of synthesis of flavonols in recent.We designed 8-mannich alkali derivatives of flavonols and their hydrochloric acid salt, In order to improve the water solubility of quercetin and kaempferol and absorption pass, we took some time to study separation and purification of mannich derivatives by TLC, because there were some outgrowths, their structure was identified by ~1H-NMR. Also, their mineral ester salts were produced throught referring to other literature, to compare of pharmacology performance.The results of experiment:We used ~1H-NMR to identify 8 mannich alkalis and 2 sulphates, which were aim production that we designed in the first. These derivatives have better water solubility, melting point higher than 300℃. The results of experiment show that mannich alkalis polarity changed to bigger. At last, the best separation condition was found that silica gel GF254, 1-butanol: water: acetic acid=4:1:1, methyl.