有机化学 ›› 2018, Vol. 38 ›› Issue (10): 2767-2774.DOI: 10.6023/cjoc201804024 上一篇    下一篇

研究简报

3-乙酰基-4-苯基-1-氧代螺[4,5]癸-3-烯-2-酮类衍生物的合成及杀菌活性

关爱莹, 赵宇, 王卫伟, 刘鑫磊, 王明安   

  1. 中国农业大学理学院应用化学系 北京 100193
  • 收稿日期:2018-04-13 修回日期:2018-05-11 发布日期:2018-06-06
  • 通讯作者: 王明安,E-mail:wangma@cau.edu.cn E-mail:wangma@cau.edu.cn
  • 基金资助:

    国家自然科学基金(No.21772229)资助项目.

Synthesis and Fungicidal Activity of 3-Acetyl-4-phenyl-1-oxaspiro[4,5]dec-3-en-2-one Derivatives

Guan Aiying, Zhao Yu, Wang Weiwei, Liu Xinlei, Wang Mingan   

  1. Department of Applied Chemistry, College of Sciences, China Agricultural University, Beijing 100193
  • Received:2018-04-13 Revised:2018-05-11 Published:2018-06-06
  • Contact: 10.6023/cjoc201804024 E-mail:wangma@cau.edu.cn
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 21772229).

将多样性导向合成策略应用于3-乙酰基-4-苯基-1-氧代螺[4,5]癸-3-烯-2-酮的羰基多样化衍生,合成了一系列结构新颖的3-乙酰基-4-苯基-1-氧代螺[4,5]癸-3-烯-2-酮衍生物.活体及离体生物活性实验结果表明,一些化合物对植物病原菌显示出优异的杀菌活性,如3-(1-烯丙氧基乙基)-4-苯基-1-氧代螺[4,5]癸-3-烯-2-酮(7)在400 μg/mL浓度下对黄瓜霜霉病和玉米锈病的抑制率均为100%.

关键词: 多样性导向合成, 3-乙酰基-4-苯基-1-氧代螺[4,5]癸-3-烯-2-酮, 杀菌活性, 植物病原菌

The diversity-orientied synthesis strategy was utilized to diversely derive from the carbonyl of 3-acetyl-4-phenyl-1-oxaspiro[4,5]dec-3-en-2-one, a series of novel 3-acetyl-4-phenyl-1-oxaspiro[4,5]dec-3-en-2-one derivatives were synthesized. The preliminary in vivo and in vitro bioassay results showed that some compounds exhibited excellent fungicidal activity against phytopathagens, such as 3-allyloxyethyl-4-phenyl-1-oxaspiro[4,5]dec-3-en-2-one (7) had 100% control rates against Pseudoperonospora cubensis and Puccinia polysora at the concentration of 400 μg/mL.

Key words: diversity-orientied synthesis, 3-acetyl-4-phenyl-1-oxaspiro[4,5]dec-3-en-2-one, fungicidal activity, phytopathagen