2-取代-3,4-二氢-1-异喹啉酮的合成及其血管舒张活性  

Synthesis of Novel 2-Subsituted-3,4-dihydro-1(2H)-isoquinolinones and Their Vasodilatation Activity

作　　者：周凯[1] 李强[1] 郑美林[1] 张三奇[1] 

机构地区：[1]西安交通大学医学院药学系,陕西西安710061

出　　处：《合成化学》2010年第3期352-355,392,共5页Chinese Journal of Synthetic Chemistry

摘　　要：以3-羟基-4,5-亚甲二氧基苯甲酸甲酯或5-羟基-1,3-苯二甲酸二甲酯为原料,经烯丙基醚化、Claisen重排、氧化、与伯胺反应(生成Schiff碱)、还原、分子内酯的酰化合成了4种新的2-取代-3,4-二氢-1-异喹啉酮(1a～1d),其结构经1HNMR和MS表征。离体动脉环张力实验证明1在浓度为1×10-4mol.L-1时具有明显舒张血管的作用。Four novel 2-substituted-3,4-dihydro-1（2H）-isoquinolinones（1a^1d）were synthesized from methyl 3-hydroxy-4,5-methylenedioxybenzoate or dimethyl 5-hydroxyisophthalate by the reaction of allyl etherification,Claisen rearrangement,oxidation,reductive amination and intramolecular amidation.The structures were characterized by 1H NMR and MS.1 exhibited the activity of vasodilatation at a concentration of 1×10-4 mol·L-1.

关 键 词：异喹啉酮 CLAISEN重排 合成 血管舒张活性 

分 类 号：O626.32[理学—有机化学] R914.5[理学—化学]