化学学报 ›› 2012, Vol. 70 ›› Issue (06): 759-764.DOI: 10.6023/A1108221 上一篇    下一篇

研究论文

哌啶并噻吩并嘧啶酮衍生物的合成、表征及生物活性

曾国平, 郑平   

  1. 湖北第二师范学院 化学与生命科学学院 武汉 430205
  • 投稿日期:2011-08-22 修回日期:2011-10-21 发布日期:2011-12-01
  • 通讯作者: 郑平
  • 基金资助:

    湖北省教育厅科研项目(No. B20113001), 湖北第二师范学院重点学科“应用化学”(No. 201008)资助项目.

Synthesis, Characterization and Biological Activity of Piperidinothienopyrimidinones

Zeng Guoping, Zheng Ping   

  1. School of Chemistry and Life Sciences, Hubei University of Education, Wuhan 430205
  • Received:2011-08-22 Revised:2011-10-21 Published:2011-12-01
  • Supported by:

    Project supported by the Hubei Province Department of Education Scientific Research (No. B20113001), Hubei University of Education Key Disciplines “Applied Chemistry” (No. 201008).

应用中间体碳二亚胺分别与伯胺、仲胺及醇在醇钠催化条件下合成9 个未见报道的新型哌啶并噻吩并嘧啶酮衍生物. 产物的结构经元素分析、1H NMR、MS 及单晶X 衍射检测得以确认. 探讨了所有化合物的杀菌活性, 结果表明部分化合物表现出较好的抑菌活性, 其中化合物7b 对黄瓜灰霉、水稻纹枯、小麦赤霉的抑制率分别为76.19%, 68.83%和56.52%.

关键词: 哌啶并噻吩并嘧啶酮, 合成, 表征, 生物活性

Nine new piperidinothienopyrimidinone derivatives were synthesized from the reaction of carbodiimide intermediate with primary, secondary amines and alcohols catalyzed by sodium alkoxide. The structures of the compound were confirmed by elemental analysis, 1H NMR, MS and single crystal X-ray determination. The fungicidal activities of all the compounds were studied and some compounds exhibited good bacteriostasis activity. Among them, compound 7b exhibited fungicidal activity against Botrytis cinereapers, Rhizoctonia solani, and Gibberella zeae with inhibitive rates of 76.19%, 68.83% and 56.52%, respectively.

Key words: piperidinothienopyrimidinone, synthesis, characterization, biological activity