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有机化学
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有机化学 ›› 2011, Vol. 31 ›› Issue (08): 1202-1207. 上一篇    下一篇

研究论文

2-[邻-4,6-二甲氧基嘧啶基-2-氧(硫)代苯基]-1,3,4-噻(噁)二唑类化合物的合成及其除草活性

张大永*,1，田庆海2，陆明若2，吴晓明1   

  1. (1中国药科大学新药研究中心 南京 210009)
    (2江苏常隆农药化工有限公司 常州 213031)
  • 收稿日期:2010-10-25 修回日期:2010-12-03 发布日期:2011-03-02
  • 通讯作者: 张大永 E-mail:zhangdayong@cpu.edu.cn

Synthesis and Herbicidal Activities of 2-(o-4,6-Dimethoxylpyrimidinyl- 2-oxo(thio)phenyl-1,3,4-thia(oxa)diazoles

Zhang Dayong*,1 Tian Qinghai2 Lu Min-gruo2 Wu Xiaoming1   

  1. (1 Center of Discovery Drug, China Pharmaceutical University, Nanjing 210009)
    (2 Jiangsu Changlong Pesticide Chemical Industry Co. Ltd., Changzhou 213031)
  • Received:2010-10-25 Revised:2010-12-03 Published:2011-03-02
  • Contact: Da-Yong ZHANG E-mail:zhangdayong@cpu.edu.cn

PDF

1337

被引次数

11

以取代的邻硝基苯甲醛或水杨醛或邻巯基苯腈为原料, 通过几步反应合成得到2-[邻-4,6-二甲氧基嘧啶-2-基-氧(硫)代苯基]-1,3,4-噻(噁)二唑类化合物. 初步田间试验证实, 30%化合物Ib乳油的使用剂量为2.40～3.60 L•hm－2, 对试验棉田杂草防除效果达48 d, 且对棉花较为安全. 目标化合物的结构经过1H NMR, MS-ESI, IR以及元素分析等表征.

关键词: 噻(噁)二唑, 乙酰乳酸合成酶(ALS), 嘧草硫醚, 除草剂, 合成

The novel compounds 2-(o-4,6-dimethoxylpyrimidinyl-2-oxo-(thio)phenyl)-1,3,4-thia(oxa) diazoles were synthesized from substituted o-nitrobenzaldehyde or salicylaldehyde and o-mercaptobenzoni- trile by several steps. The employment dosage of 30% compound Ib was 2.40～3.60 L•hm－2, the rudiment cotton field herbicidal activities were over 48 d, and could lead to further research. The structures of target compounds were identified by IR, 1HNMS, MS techniques and elemental analysis.

Key words: thia(oxa)diazole, acetolactate synthetase, pyrithiobac-sodium, herbicide, synthesis