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有机化学
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有机化学 ›› 2011, Vol. 31 ›› Issue (08): 1240-1244. 上一篇    下一篇

研究论文

3-CH2CH2COOCH3取代的1,5-苯并硫氮杂衍生物的合成、晶体结构及抑菌活性研究

张萍1，宣烨1，刘薇2，李媛*,1   

  1. (1河北师范大学化学与材料科学学院 石家庄 050016)
    (2河北师范大学生命科学学院 石家庄 050016)
  • 收稿日期:2010-11-10 修回日期:2011-03-01 发布日期:2011-03-29
  • 通讯作者: 李媛 E-mail:yuanli@mail.hebtu.edu.cn

Synthesis, Crystal Structure and Antibacterical Properties of 3-CH2CH2COOCH3 Substi-tuted 1,5-Benzothiazepines

Zhang Ping1 Xuan Ye1 Liu Wei2 Li Yuan*,1   

  1. (1 College of Chemistry, Hebei Normal University, Shijiazhuang 050016)
    (2 College of Life Science, Hebei Normal University, Shijiazhuang 050017)
  • Received:2010-11-10 Revised:2011-03-01 Published:2011-03-29

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从不同取代的苯出发, 经5步反应合成了一系列3-CH2CH2COOCH3取代的1,5-苯并硫氮杂衍生物. 化合物的结构经IR, 1H NMR, 13C NMR, MS和元素分析确证, 并用X射线单晶衍射测定了化合物5f的晶体结构, 证实了分子中的七元杂环是类船式构象. 初步的抑菌活性测试结果表明, 化合物5f和5h对枯草芽孢杆菌和临床新生隐球菌有微弱的抑制作用.

关键词: 1,5-苯并硫氮杂, 晶体结构, 抑菌活性

Starting from substituted benzenes, a series of 3-CH2CH2COOCH3 substituted 1,5-benzothi- azepines were synthesized through 5-step reactions. The structures of the new products were confirmed by IR, 1H NMR, 13C NMR, MS techniques and elemental analysis. The crystal structure of the compound 5f has been deterimined by X-ray diffraction analysis and the conformation of the seven-membered heterocycle is boat-like. The preliminary antibacterical experimental results showed that 5f and 5h have weak activities to Bacillus subtilis and Cryptococcus neoformansis.

Key words: 1,5-benzothiazepine, crystal structure, antibacterical propertiy