Chin. J. Org. Chem. ›› 2015, Vol. 35 ›› Issue (5): 1166-1172.DOI: 10.6023/cjoc201410041 Previous Articles     Next Articles



阮铃莉a, 范人杰a, 刘幸海a, 陈杰b, 翁建全a   

  1. a 浙江工业大学化学工程学院 杭州 310032;
    b 国家南方农药创制中心浙江基地生测部 杭州 310023
  • 收稿日期:2014-10-31 修回日期:2014-12-14 发布日期:2015-01-07
  • 通讯作者: 翁建全
  • 基金资助:


Synthesis and Antifungal Activity of Novel 3-[(5-Benzylthio- 1,3,4-oxadiazol-2-yl)methyl]benzo[d]thiazol- (oxazol)-2(3H)-ones

Ruan Linglia, Fan Renjiea, Liu Xinghaia, Chen Jieb, Weng Jianquana   

  1. a College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310032;
    b Bioassay Department, Zhejiang Branch of National Southern Pesticide Research Centre, Hangzhou 310023
  • Received:2014-10-31 Revised:2014-12-14 Published:2015-01-07
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No.30900959) and Public Project of Zhejiang Province (No.2014C31127).

In order to find novel biologically active pesticide lead compounds, twenty-one novel 3-[(5-benzylthio-1,3,4- oxadiazol-2-yl)methyl]benzo[d]thiazol(oxazol)-2(3H)-ones were synthesized by 2-benzothiazolinone/benzoxazolone as starting materials via substitution, hydrazine, cyclization and the last benzylation reaction. The structures of the title compounds were characterized by 1H NMR, IR, EI-MS and elemental analysis. The preliminary bioassay results indicated that most of them showed moderate inhibition activity against Colletotrichum orbiculare, Botrytis cinerea and Rhizoctonia solani at 50 mg/L, and the inhibition rate of compound 5b against Botrytis cinerea and Rhizoctonia solani reached above 85%.

Key words: 2-benzothiazolinone/benzoxazolone, thioether, 1,3,4-oxadiazole, microwave synthesis, antifungal activity