3-O-甲基槲皮素的合成  

Facile Synthesis of 3-O-Methylquercetin

作　　者：李化军[1] 栾新慧[1] 赵毅民[1] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850

出　　处：《有机化学》2004年第12期1619-1621,共3页Chinese Journal of Organic Chemistry

基　　金：国家 8 63基金 (No.2 0 0 2AA2Z31 31 )资助项目

摘　　要：以芦丁为原料经苄基化、酸水解、选择性甲基化和氢化脱苄四步反应 ,合成了 3 O 甲基槲皮素 ,总收率为 76% .利用1HNMR和MS对中间体及产物的结构进行了确证 .该发现有望为 3 取代槲皮素衍生物的合成提供一条捷径 .3-O-Methylquercetine, a 3-O-methyl-3',4',5,7-tetrahydroxylflavone, was synthesized from commercially low-cost rutin in 76% overall yield and in four steps, i. e. selective benzylation of rutin, hydrolysis of glycosidic bond, regioselective methylation of 3-OH and cleavage of the benzyl group by hydrogenolysis. The structures of intermediates and the product were comfirmed by H-1 NMR and MS spectra. This finding prospected to provide a shortcut to the synthesis of 3-substituted quercetin derivatives.

关 键 词：甲基化 合成 总收率 氢化 苄基化 中间体 取代 槲皮素 芦丁 MS 

分 类 号：O629[理学—有机化学]