槲皮素衍生物的8位对甲苯基硫醚化反应研究

摘要

槲皮素属于黄酮类化合物,具有广泛的生理活性.硫代黄酮类化合物有良好的生物活性,然而目前仅有两种碳-硫取代黄酮类化合物的合成方法.近年来发现,磺酰肼由于其容易制备、无味、较稳定等优点而成为一种新颖的环境友好的硫醚化试剂.本文以对甲苯磺酰肼为硫化试剂,通过调节槲皮素上烷基保护基的种类和个数实现槲皮素8位区域选择性对甲苯基硫醚化,并探讨了不同保护基对反应产率的影响.%Quercetin is a kind of flavonoid which displays a wide variety of pharmacological activities.As we know that sulfur substituted flavonoids have good bioactivities,but currently only two methods have been reported for synthesizing flavonoid thioether by direct sulfenylation.Sulfonyl hydrazides have been developed as novel and environmentally friendly sulfenylation reagents that are stable,readily accessible and odor-free.In this research,we completed 8-thiolation of quercetin derivative with regio-selectivity by using p-toluenesulfonyl hydrazide via alternating alkyl protecting groups.In addition,the effect of different protecting groups on the reaction yield was also studied.