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Chin. J. Org. Chem. ›› 2008, Vol. 28 ›› Issue (2): 317-320. Previous Articles     Next Articles

Reports

1,5-苯并二氮杂的合成及其生物活性研究

刘进兵，林崇懒，万一千，宋化灿*   

  1. (中山大学化学与化学工程学院 广州 510275)
  • 收稿日期:2007-04-08 修回日期:2007-05-30 发布日期:2008-02-01
  • 通讯作者: 宋化灿

Synthesis and Bioactivities of 1,5-Benzodiazepine Derivatives

LIU Jin-Bing,LIN Chong-Lan,WAN Yi-Qian,SONG Hua-Can*   

  1. (School of Chemistry and Chemical Engineering, Sun Yat-Sen University, Guangzhou 510275)
  • Received:2007-04-08 Revised:2007-05-30 Published:2008-02-01
  • Contact: SONG Hua-Can*

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1,5-Benzodiazepine derivatives were synthesized by two different methods: the reaction of chalcone with benzene-1,2-diamine in aluminum oxide under solvent-free conditions and one-pot reaction of substituted-acetophenones with benzene-1,2-diamine in the presence of PPA (polyphosphoric acid) as cata-lyst with the yields of 53.7%～73.57%. They were characterized by 1H NMR, 13C NMR, MS, IR spectra and elemental analysis and evaluated against bacteria and acetylcholinesterase.

Key words: synthesis, benzodiazepine, bioactivities