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Chin. J. Org. Chem. ›› 2009, Vol. 29 ›› Issue (12): 2000-2004. Previous Articles     Next Articles

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2-[4-(2,6-二氟苯基)噻唑-2-基]-3-羟基丙烯腈衍生物的合成及生物活性

杨 鹏*,a；翁建全b；谭成侠b；王秀莲a   

  1. 杨 鹏*,a；翁建全b；谭成侠b；王秀莲a
  • 收稿日期:2009-03-15 修回日期:2009-05-20 发布日期:2009-07-10
  • 通讯作者: 杨鹏 E-mail:yangpenghz@126.com
  • 基金资助:

    浙江省自然科学基金;国家级.国家自然科学基金

Synthesis and Biological Activities of 2-(4-(2,6- Difluorophenyl)thiazol)-2-yl)-3-Hydroxy Acrylonitrile Derivatives

Yang, Peng*,a；Weng, Jianquanb；Tan, Chengxiab；Wang, Xiuliana   

  1. (a Qianjiang College, Hangzhou Normal University, Hangzhou 310012) (b College of Chemical Engineering and Materials Science, Zhejiang University of Technology, Hangzhou 310014)
  • Received:2009-03-15 Revised:2009-05-20 Published:2009-07-10

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In order to find thiazolylacrylonitriles with good biological activities, eight 2-[4-(2,6-difluoro phenyl)thiazol-2-yl]-3-hydroxy-3-alkoxyl(aryloxy)acrylonitriles (5) and seven 2-[4-(2,6-difluorophenyl) thiazol-2-yl]-3-hydroxy-3-arylamineacrylonitriles (7), all of which were reported for the first time, were synthesized by the reaction of 2-[4-(2,6-difluorophenyl)thiazol-2-yl]acetonitrile (3) with substituted chloro-formates 4 and aryl isocyanates 6 in the presence of base. Their structures were confirmed by 1H NMR, IR, MS data and elemental analysis. The preliminary bioassay showed that all compounds had certain fungicidal and insecticidal activities. The inhibition rates of compounds 5f and 5h were above 95% against Colle-totrichum gossypii at 100 mg/L, and the mortality rates of compounds 5g and 7d were above 85% against Tetranychus urticae at 250 mg/L.

Key words: 2-[4-(2,6-difluorophenyl)thiazol-2-yl]acetonitrile, thiazolylacrylonitrile, synthesis, biological activity

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