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有机化学
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有机化学 ›› 2011, Vol. 31 ›› Issue (11): 1878-1883. 上一篇    下一篇

研究论文

豆腐果苷-喹啉和黄酮衍生物的合成及镇静活性研究

陈超，李霞，胡晓枫，李颖，尹述凡*   

  1. (四川大学化学学院 成都 610064)
  • 收稿日期:2011-03-28 修回日期:2011-04-29 发布日期:2011-06-21
  • 通讯作者: 尹述凡 E-mail:chuandayouji217@163.com;;

Synthesis and Calm Activity of Quinoline and Flavone Derivatives of Helicid

CHEN Chao, LI Xia, HU Xiao-Feng, LI Ying, YIN Shu-Fan   

  1. (College of Chemistry, Sichuan University, Chengdu 610064)
  • Received:2011-03-28 Revised:2011-04-29 Published:2011-06-21

PDF

1006

被引次数

25

以L-脯氨酸为有机催化剂一步合成了豆腐果苷-喹啉酮(2), 在此基础上合成了一系列豆腐果苷-喹啉衍生物3a～3c, 4和5a～5c|以苄溴、豆腐果苷、邻羟基苯乙酮, 氨基脲盐酸盐、羟胺盐酸盐、甲氧基胺盐酸盐为原料合成出豆腐果苷-黄酮衍生物8和9a～9c. 产物结构经1H NMR, IR和HRMS确认. 初步生物活性测试结果表明5b和9b具有较好的镇静催眠活性.

关键词: 豆腐果苷, 喹啉, 黄酮, 镇静催眠

Helicid-quinoline 2 was synthesized by using L-proline as an effective organocatalyst in one step, and a series of quinoline derivatives 3a～3c, 4 and 5a～5c were obtained from 2. Helicid-flavone derivatives 8 and 9a～9c were conveniently prepared from benzyl bromide, helicid, 2-hydroxyacetophenone, semicarbazide hydrochloride, hydroxylamine hydrochloride and methoxy amine hydrochloride as the start-ing materials. Their chemical structures were con?rmed by 1H NMR, IR and HRMS tech-niques. The bioassay test results showed that 5b and 9b had good calm activity.

Key words: helicid, quinoline, flavone, hypnotic-sedative