Chin. J. Org. Chem. ›› 2013, Vol. 33 ›› Issue (02): 353-358.DOI: 10.6023/cjoc201208033 Previous Articles     Next Articles



林选福, 谭赞, 刘勇, 贺银菊, 鲍小平   

  1. 贵州大学精细化工研究开发中心 教育部绿色农药与农业生物工程重点实验室 贵阳 550025
  • 收稿日期:2012-08-29 修回日期:2012-10-15 发布日期:2012-10-24
  • 通讯作者: 鲍小平
  • 基金资助:

    贵州省优秀科技教育人才省长专项资金(No. 200817)资助项目.

Synthesis and Fungicidal Activities of 2-Benzylthio(sulfonyl)-5- methyl-7-substituted benzyloxy-1,2,4-triazolo[1,5-a] pyrimidine Derivatives

Lin Xuanfu, Tan Zan, Liu Yong, He Yinju, Bao Xiaoping   

  1. Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025
  • Received:2012-08-29 Revised:2012-10-15 Published:2012-10-24
  • Supported by:

    Project supported by the Governor’s Foundation for Excellent Talents of Science, Technology & Education of Guizhou Province (No. 200817).

Using 2-benzylthio-5-methyl-7-hydroxyl-1,2,4-triazolo[1,5-a]pyrimidine as starting material, twelve novel 2-benzylthio-5-methyl-7-substituted benzyloxy-1,2,4-triazolo[1,5-a]pyrimidine derivatives 5a5l and their sulfonyl analogues 6a6l were synthesized through sequential reactions of etherification and oxidation, respectively. Their structures were characterized by 1H NMR, IR, MS and elemental analysis. The preliminary bioassay indicated that some compounds exhibited certain fungicidal activities, for example, the inhibition rates of compounds 5c, 5k and 5l (50 μg/mL) against Botrytis cinerea were 61%, 69% and 85%, respectively.

Key words: 1,2,4-triazolo[1,5-a]pyrimidine, thioether (sulfone), oxygen ether, synthesis, fungicidal activity