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有机化学
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有机化学 ›› 2006, Vol. 26 ›› Issue (08): 1106-1110. 上一篇    下一篇

研究简报

N-取代苯基-2-取代-1,3-噻唑烷-3-甲酰胺的合成、结构及生物活性

翁建全*,1，沈德隆1，谭成侠1，欧晓明2   

  1. (1浙江工业大学化学工程与材料学院 杭州 310032)
    (2国家南方农药创制中心湖南基地生测部 长沙 410007)
  • 收稿日期:2005-11-17 修回日期:2006-02-17 发布日期:2006-07-26
  • 通讯作者: 翁建全

Synthesis, Structure and Biological Activities of N-Arylaminocarbonyl-2-oxo/thio-thiazolidine

WENG Jian-Quan*,1,SHEN De-Long1,TAN Cheng-Xia1,OU Xiao-Ming2   

  1. (1 College of Chemical Engineering and Materials Science, Zhejiang University of Technology, Hangzhou 310032)
    (2 Bioassay Department, Hunan Branch of National Southern Pesti-cide Research Centre, Changsha 410007)
  • Received:2005-11-17 Revised:2006-02-17 Published:2006-07-26
  • Contact: WENG Jian-Quan

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为了寻找新的含噻唑杂环的先导化合物, 利用2-取代-1,3-噻唑烷与取代苯基异氰酸酯在三乙胺催化下发生偶合反应, 合成了17个N-取代苯基-2-取代-1,3-噻唑烷-3-甲酰胺化合物3, 并利用1H NMR, IR, MS和元素分析对其结构进行了表征. 用X-ray单晶衍射测定了N-苯基-2-氧代-1,3-噻唑烷-3-甲酰胺(3a)的晶体结构. 初步生物活性试验结果表明, 在试验浓度下部分目标化合物具有一定的杀菌和杀虫活性.

关键词: 2-取代-1,3-噻唑烷, 生物活性, 取代苯基异氰酸酯, 结构, 合成

In order to find new thiazole-heterocycle lead compounds, seventeen N-arylaminocarbonyl-2- oxo/thio-thiazolidine derivatives were synthesized from a coupling reaction of 2-oxo/thio-thiazolidine and aryl isocyanates catalyzed by Et3N. Their structures were confirmed by 1H NMR, IR, MS spectra and elemental analysis. The crystal structure of N-anilinocarbonyl-2-oxothiazolidine was determined by X-ray diffraction analysis. The preliminary bioassay showed that some of them exhibited certain fungicidal and insecticidal activities.

Key words: substituted phenyl isocyanate, biological activity, synthesis, structure, 2-oxo/thio-thiazolidine