Synthesis Of Betulin Ester Of Coumarin-3-Caboxylic Acid And Gallic Acid

Birch trees in shangbai Mountain, Jilin province of China is rich in resources, widespread concern in the pharmacological effects of birch bark was, Chemical composition of birch bark complex, Betulin, betulinic acid and many of their derivatives exhibit great promise for the treatment of HIV infection,cancer and Anti-inflammatory. Several countries have already has extensive research into the chemical composition of birch bark, Birch in the result indicates that it is rich in Betulin and part of betulinic acid. Study on Birch resources, natural medicine research is of great significance.Betulin and betulinic acid are remarkable natural products. They are obtained from a variety of botanical sources. Since1995, betulinic acid against cultured human melanoma cells has recently been discovered to possess antitumor activity and selectivity, betulinic acid was known as a very promising anticancer drug candidate. Betulin, a naturally occurring triterpene, available in abundance up to13%dry weight of bark from white birch bark seems to be an ideal starting material for the synthesis of betulinic acid. Betulin relative advantages of betulinic acid modified with three points, looked after the modification activity strengthened. During a discovery effort from natural resources betulin. we design synthesis and natural extracts from birch bark, Betulin. Parallel structure modification of a certain activity of small molecules such as coumarin-3-carboxylic acid and gallic acid, we synthesized some derivatives of betulin with modifications at the positions C-3and C-28. In order to seek new biologically active compounds reduce side effects and improve water solubility. Direct reaction of betulin with coumarin-3-carboxylic acid or gallic acid led to betulin-28-esters and betulin-3,28-diesters. These betulin-3-esters were synthesized through protection, esterification and deprotection steps using betulin as a starting material. Their structures were confirmed by IR.,1H-NMR and1C-NMR. The esters of coumarin-3-carboxylic acid were tested in vitro for their inhibitory activity.