📜6,8-Dibromo-3,7-O-Dimethyltamarixetin置于palladium 10% On Activated Carbon,氢气体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,20.0 °C,101.33 Kpa 条件下,反应 48.0H,以73%的收率获得产物5,3'-二羟基-3,7,4'-三甲氧基黄酮
参考文献:Semisynthesis Of Natural Flavones Inhibiting Tubulin Polymerization,From Hesperidin
标题:Semisynthesis Of Natural Flavones Inhibiting Tubulin Polymerization,From Hesperidin
摘要:Semisynthesis Of 5,3'-Dihydroxy-3,6,7,8,4'-Pentamethoxyflavone (1),A Natural Flavone That Binds With High Affinity To Tubulin,Was Performed From Hesperidin,The Very Abundant Citrus Flavanone,By A Five-Step Sequence. The Last Step Of The Synthesis Also Gave Rise To 5,3'-Dihydroxy-3,6,7,4'-Tetramethoxyflavone (= Casticin Or Vitexicarpin) (10),5,3'-Dihydroxy-3,7,8,4'-Tetramethoxyflavone (= Gossypetin 3,7,8,4'-Tetramethyl Ether) (11),And,Unexpectedly,5,7,3'-Trihydroxy-3,6,8,4'Tetramethoxyflavone (12) And 5,3'-Dihydroxy-8-Dimethylamino-3,6,7,4'-Tetramethoxyflavone (= 8-Dimethylaminocasticin) (13). Cytotoxicity And Antitubulin Activity Of These Five Flavones,As Well As 5,3'-Dihydroxy-3,7,4'-Trimethoxyflavone (= Ayanin) (14) And Intermediate 6,8-Dibromo-Ayanin (8),Were Evaluated. Comparison Of The Responses Confirmed And Clarified The Influence Of The A-Ring Substitution Pattern On The Biological Activity.
DOI:10.1021/np100065V