有机化学 ›› 2019, Vol. 39 ›› Issue (3): 836-841.DOI: 10.6023/cjoc201809009 上一篇    下一篇

研究简报

新型哌啶噻唑类化合物的合成及杀虫活性

丁成荣, 潘亚运, 殷许, 谭成侠, 张国富   

  1. 浙江工业大学 杭州 310032
  • 收稿日期:2018-09-05 修回日期:2018-10-22 发布日期:2018-11-26
  • 通讯作者: 谭成侠, 张国富 E-mail:tanchengxia@zjut.edu.cn;gfzhang@zjut.edu.cn
  • 基金资助:

    浙江省绿色农药2011协同创新中心开放基金资助项目.

Synthesis and Insecticidal Activity of Novel Piperidine Thiazole Compounds

Ding Chengrong, Pan Yayun, Yin Xu, Tan Chengxia, Zhang Guofu   

  1. College of Chemical Engineering and Materials Science, Zhejiang University of Technology, Hangzhou 310032
  • Received:2018-09-05 Revised:2018-10-22 Published:2018-11-26
  • Contact: 10.6023/cjoc201809009 E-mail:tanchengxia@zjut.edu.cn;gfzhang@zjut.edu.cn
  • Supported by:

    Project supported by the Collaborative Innovation Center of Zhejiang Province Green Pesticide.

为了探寻新型的生物活性化合物,设计并合成了12个未见文献报道的新型哌啶噻唑类衍生物.生物活性测试研究发现,在500 μg/mL浓度下,目标化合物对粘虫表现出良好的抑制活性,而且在100 μg/mL下,(4-(5-(3-氯苯基)-4-甲基噻唑-2-基)哌啶-1-基)(4-甲基哌嗪-1-基)甲酮(1f)、(5-(3-氯苯基)-4-甲基噻唑-2-基)哌啶-1-基)(4-硝基-1H-吡唑-3-基)甲酮(1g)对粘虫的抑制率均达80%以上,另外在20 μg/mL下(5-(3-氯苯基)-4-甲基噻唑-2-基)哌啶-1-基)(4-硝基-1H-吡唑-3-基)甲酮(1g)仍具有50%的杀虫活性.

关键词: 氟噻唑吡乙酮, 哌啶噻唑类衍生物, 杀虫活性

Twelve new piperdine thiazole compounds were designed and synthesized in search of new bioactive compounds. The preliminary bioassay showed that at the concentration of 500 μg/mL the lethal rates of the target compounds possessed certain insceticidal activities against armyworm, and at the concentration of 100 μg/mL the lethal rates of (4-(5-(3-chloro-phenyl) -4-methylthiazol-2-yl) piperidin-1-yl) (4-methylpiperazin-1-yl) methanone (1f) and (4-(5-(4-chlorophenyl) -4-methyl-thiazol-2-yl) piperidin-1-yl) nitro-1H-pyrazol-3-yl) methanone (1g) against armyworm were 80% and 100%, respectively. Further screening at concentrations of 20 μg/mL, the lethal rate of (4-(5-(4-chlorophenyl) -4-methylthiazol-2-yl) piperidin-1-yl) (4-nitro-1H-pyrazol-3-yl) methanone (1g) against armyworm was 50%.

Key words: oxathiapiprolin, piperidine-thiazolederivatives, insecticidal activity