Chin. J. Org. Chem. ›› 2009, Vol. 29 ›› Issue (06): 966-970. Previous Articles     Next Articles

Reports

2-取代-3,4-二氢-1-异喹啉酮的合成和舒张血管活性

张三奇*,a; 李 强a ; 祝丽永b ; 曹永孝a; 刘瑞熙a ; 陈战国b   

  1. (a西安交通大学医学院 西安710061)
    (b陕西师范大学化学与材料科学学院 西安710062)
  • 收稿日期:2008-05-13 修回日期:2008-12-10 发布日期:2009-06-20
  • 通讯作者: 张三奇

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

Zhang, Sanqi*,a; Li, Qiang a; Zhu, Liyong b; Cao, Yongxiaoa ;
Liu, Ruixia; Chen, Zhanguob
  

  1. (a School of Medicine, Xi’an Jiaotong University, Xi’an 710061)
    (b College of Chemistry & Materials Science, Shanxi Normal University, Xi’an 710062)
  • Received:2008-05-13 Revised:2008-12-10 Published:2009-06-20
  • Contact: Zhang, Sanqi

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.

Key words: Claisen rearrangement, one-pot method, vasodilatati, isoquinolinone