2-取代-3,4-二氢-1-异喹啉酮的合成和舒张血管活性

以3-羟基-4-甲氧基苯甲酸甲酯等为原料, 通过烯丙基醚化、Claisen重排、氧化、与伯胺反应(生成Schiff碱)、还原、分子内酯的胺解六步反应合成了一系列2-取代-3,4-二氢-1-异喹啉酮类化合物. Schiff碱的制备、还原、酯的胺解三步在“一锅”内完成. 采用1H NMR, MS和元素分析对目标化合物的结构进行了表征. 离体动脉环张力实验证明此类化合物具有明显舒张血管的作用.

Synthesis and Vasodilatation of 2-Substituted-3,4- dihydro-1(2H)-isoquinolinones

2-Substituted-3,4-dihydro-1(2H)-isoquinolinones were synthesized from methyl 3-hydroxy-ben- zoates via allyl etherification, Claisen rearrangement, oxidation, reductive amination and aminolysis for the first time. The three steps, imine-formation, reduction and intramolecular amidation, were completed in one-pot at room temperature. The structures of the title compounds were characterized by 1H NMR, MS techniques and elemental analyses. Further more, myograph pharmacology methods demonstrated that several products exhibited the activity of vasodilatation.