有机化学 ›› 2005, Vol. 25 ›› Issue (9): 1053-1056. 上一篇    下一篇

研究论文

N′-(取代嘧啶-2-基)-N-菊酰硫脲的合成与生物活性研究

许东芳,李景智,郭彦玲,柯少勇,薛思佳*   

  1. (上海师范大学生命与环境科学学院化学系 上海 200234)
  • 收稿日期:2004-06-24 修回日期:2004-03-21 发布日期:2005-08-24
  • 通讯作者: 薛思佳

Synthesis and Biological Activity of N'-(substituted pyrimidin-2-yl)- N-chrysanthemoylthiourea Derivatives

XU Dong-Fang,LI Jing-Zhi,GUO Yan-Ling,KE Shao-Yong,XUE Si-Jia*   

  1. (Department of Chemistry, Shanghai Normal University, Shanghai 200234)
  • Received:2004-06-24 Revised:2004-03-21 Published:2005-08-24
  • Contact: XUE Si-Jia

采用活性基团拼接法, 将第一菊酸构型中的最高活性组分(+)-反式菊酸以及二氯菊酸引入到含取代嘧啶环的酰基硫脲结构中, 合成了5个未见文献报道的N′-(取代嘧啶-2-基)-N-(+)-反式菊酰硫脲衍生物(3a3e)和3个均未见文献报道的N′-(取代嘧啶-2-基)-N-二氯菊酰硫脲(3f3h), 结构经元素分析、IR和1H NMR得到确证. 初步的生物活性测试结果表明: 大部分化合物具有较好的杀菌活性, 有的化合物兼具除草和杀菌活性, 有的化合物兼具杀虫和杀菌活性.

关键词: N'-(取代嘧啶-2-基)-N-(+)-反式菊酰硫脲, N′-(取代嘧啶-2-基)-N-二氯菊酰硫脲, 生物活性, 合成

Five new N′-(substituted pyrimidin-2-yl)-N-chrysanthemoylthiourea derivatives and three new N′-(substituted pyrimidin-2-yl)-N-dichlorochrysanthemoylthiourea derivatives have been synthesized and characterized. The structures of these compounds were conformed by 1H NMR, IR spectra and elemental analysis. The preliminary biological tests showed that some of these target compounds have excellent biological activity.

Key words: N′-(substituted pyrimidin-2-yl)-N-chrysanthemoylthiourea, synthesis, biological activity, N′-(substituted pyrimidin-2-yl)-N- dichlorochrysanthemoylthiourea