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有机化学
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有机化学 ›› 2006, Vol. 26 ›› Issue (9): 1264-1267. 上一篇    下一篇

研究简报

[α-(2-氧代烷基)-α-(取代苯胺基)甲基苯基]-β-D-吡喃阿洛糖苷的合成及镇静活性研究

祝钱莉，唐强，李颖，尹述凡*   

  1. (四川大学化学学院 成都 610064)
  • 收稿日期:2005-12-06 修回日期:2006-01-08 发布日期:2006-09-11
  • 通讯作者: 尹述凡

Synthesis and Calm Activity of [α-(2-Oxoalkyl)-α-(substitutedAnilimo) me-thyl]phenyl-β-D-allopyranoside

ZHU Qian-Li,TANG Qiang,LI Ying,YIN Shu-Fan*   

  1. (Faculty of Chemistry, Sichuan University, Chengdu 610064)
  • Received:2005-12-06 Revised:2006-01-08 Published:2006-09-11
  • Contact: YIN Shu-Fan

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以豆腐果苷为原料, 通过Mannich反应与取代苯胺和脂肪酮共合成了七个豆腐果苷衍生物, 均未见文献报道. 其结构经1H NMR, IR, MS和HRMS确认, 并进行了药理活性筛选. 结果表明, 部分化合物均具有良好的镇静活性. 其中, 化合物2a (200 mg/kg), 2b (200 or 100 mg/kg)和2e (200 mg/kg)与豆腐果苷相比较, 具有更强的疗效.

关键词: 豆腐果苷, Mannich碱, 镇静活性, 合成

Seven novel helicid derivatives have been designed and synthesized by the Mannich reaction of helicid with substituted aniline and aliphatic ketone. The structures of all these new compounds were characterized by 1H NMR, IR, MS and HRMS spectra. The preliminary bioassay test suggested that some of such compounds should show good calm activity. For example, compounds 2a (200 mg/kg), 2b (200 or 100 mg/kg) and 2e (200 mg/kg) are more effective than the parent helicid.

Key words: Mannich base, synthesis, calm activity, helicide