Chin. J. Org. Chem. ›› 2007, Vol. 27 ›› Issue (06): 753-757. Previous Articles     Next Articles

Original Articles

3-取代苄基-6-三氟甲基嘧啶-2,4(1H,3H)-二酮衍生物的合成及其除草活性的研究

朱有全,邹小毛*,李公春,姚昌盛,司学凯,杨华铮*   

  1. (南开大学元素有机化学国家重点实验室及元素有机化学研究所 天津 300071)
  • 收稿日期:2006-07-14 修回日期:2006-08-29 发布日期:2007-05-21
  • 通讯作者: 邹小毛

Synthesis and Herbicidal Evaluation of 3-Substituted Benzyl-6- (trifluoromethyl)pyrimidine-2,4(1H,3H)-dione Deriva-tives

ZHU You-Quan, ZOU Xiao-Mao*, LI Gong-Chun, YAO Chang-Sheng
SI Xue-Kai, YANG Hua-Zheng*   

  1. (State Key Laboratory of Elemento-organic Chemistry, Institute of Elemento-organic Chemis-try,
    Nankai University, Tianjin 300071)
  • Received:2006-07-14 Revised:2006-08-29 Published:2007-05-21
  • Contact: YANG Hua-Zheng

In order to further study the herbicidal activity of 3-substituted benzyl-6-(trifluoro- methyl)pyrimidine-2,4(1H,3H)-dione derivatives and find new herbicides, sixteen new 3-substituted benzyl-6-(trifluoromethyl)pyrimidine-2,4(1H,3H)-dione derivatives were syn-thesized and confirmed by 1H NMR, IR spectra and elemental analysis. The bioassay results showed that the title compounds herbicidal activity, selectivity and action mode were influenced by the sub-stituent at 1-position for pyrimidine ring. Quantitative structure-activity relationship studies showed that when the test grass was rape, their herbicidal activity was mainly related with substituent molar refractivity (MR); when the test grass was barnyard grass, their herbicidal activity was mainly related with the electronic parameters of the substituents at the para-position of benzene ring. When the substituent at 1-position for pyrimidine ring was hydrogen, the inhibition against rape was improved, while when the substituent at 1-position for pyrimidine ring was methyl group, the inhibition against barnyard grass was improved.

Key words: 6-(trifluoromethyl)pyrimidine-2,4(1H,3H)-dione, quantitative structure-activity relationship, herbicide