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有机化学 ›› 2005, Vol. 25 ›› Issue (02): 197-200. 上一篇    下一篇

研究论文

2-(1-苯基/取代苯基-3-甲基-5-氯-1H-4-吡唑基)-3-芳酰胺-4-噻唑啉酮的合成及生物活性

文丽荣1，李明*,1,2，景淑霞1，曹玮1，杨华铮*,2   

  1. (1 青岛科技大学化学与分子工程学院 青岛 266042)
    (2 南开大学元素有机化学国家重点实验室 天津 300071)
  • 收稿日期:2004-05-10 修回日期:2004-09-13 发布日期:2005-01-15
  • 通讯作者: 杨华铮

Synthesis and Biological Activities of 2-(1-Aryl-3-methyl-5-chloro-1H-pyrazol-4-yl)-3-(1-aroylamino)-4-thiazolidinones

WEN Li-Rong1,LI Ming*,1,2,JING Shu-Xia1,CAO Wei1,YANG Hua-Zheng*,2   

  1. (1 College of Chemical and Molecular Technology, Qingdao University of Science and Technol-ogy, Qingdao 266042)
    (2 Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071)
  • Received:2004-05-10 Revised:2004-09-13 Published:2005-01-15
  • Contact: YANG Hua-Zheng

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利用1-芳基-3-甲基-5-氯-1H-4-吡唑醛(2)分别与取代苯甲酰肼反应, 进一步与巯基乙酸关环, 合成了11个新的2-(1-芳基-3-甲基-5-氯-1H-4-吡唑基)-3-芳酰胺-4-噻唑啉酮类化合物 3a～3k, 并利用元素分析, IR, 1H NMR和X-ray晶体衍射确定了其结构. 初步生物活性表明: 3e具有杀菌活性, 3e和3k具有除草活性.

关键词: 吡唑衍生物, 噻唑啉酮, 合成, 生物活性

By the reactions of 1-aryl-3-methyl-5-chloro-1H-4-pyrazolylformaldehydes (2) with aroylhydrazines and followed by the addition of mercaptoacetic acid, eleven new compounds 2-(1-aryl-3-methyl-5-chloro-1H-pyrazol-4-yl)-3-(1-aroylamino)-4-thiazolidinones 3a～3k have been synthesized. Their structures were characterized by elemental analysis, IR and 1H NMR spectra, and one of them 3d by X-ray diffraction study. The preliminary bioassay tests showed that compound 3e possessed moderate fungicidal activity and 3e and 3k only exhibited certain herbicidal activity.

Key words: thiazolidinone, pyrazole derivative, synthesis, biological activity