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有机化学
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有机化学 ›› 2008, Vol. 28 ›› Issue (2): 317-320. 上一篇    下一篇

研究简报

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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采用两种方法: 以三氧化铝为载体邻苯二胺与查尔酮为原料的无溶剂合成法和以PPA(多聚磷酸)为催化剂邻苯二胺与苯乙酮的一锅合成法, 合成了1,5-苯并二氮杂, 产物收率为53.7%～74.5%. 通过1H NMR, 13C NMR, MS, IR, 元素分析等手段对所合成的化合物进行了结构确定, 并测试了它们对菌和乙酰胆碱酶的抑制活性.

关键词: 苯并二氮杂, 合成, 生物活性

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