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3-取代苄氧基-6-(取代-1H-吡唑-1-基)哒嗪的合成与生物活性

Synthesis and Biological Activity of 3-(Substituted benzyloxy)-6-[(un)substituted 1H-prazol-1-yl]pyridazines

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【作者】 胡方中张桂峰邹小毛刘斌朱有全杨华铮

【Author】 HU,Fang-Zhong ZHANG,Gui-Feng ZOU,Xiao-Mao LIU,Bin ZHU,You-Quan YANG,Hua-Zheng (State Key Laboratory of Elemento-Organic Chemistry,Institute of Elemento-Organic Chemistry, Nankai University,Tianjin 300071)

【机构】 南开大学元素有机化学国家重点实验室元素有机化学研究所

【摘要】 3-氯-6-肼基哒嗪分别与乙酰丙酮和3-二甲胺基丙烯醛反应,合成了中间体3-氯-6-(3,5-二甲基-1H-吡唑-1-基)哒嗪(2)和3-氯-6-(1H-吡唑-1-基)哒嗪(4),它们与多种取代苄醇反应,得到了一系列未见报道的3-取代苄氧基-6-(取代-1H吡唑-1-基)哒嗪,其结构均经1HNMR,IR和元素分析确证.初步的生物活性测试结果表明,所合成的化合物对油菜和稗草均具有一定的抑制作用.

【Abstract】 A series of novel 3-(substituted benzyloxy)-6-[(un)substituted 1H-pyrazol-1-yl] pyridazine de-rivatives were synthesized through the condensation of various substituted benzyl alcohols with 3-chloro-6-(3,5-dimethyl-1H-pyrazole-1-yl)pyridazine(2) or 3-chloro-6-(1H-pyrazol-1-yl)pyridazine(4).2 and 4 were obtained from the cyclization of 3-chloro-6-hydrazinylpyridazine with acetoacetone and/or 3-dimethylamino acrolein.The structures of the title compounds were identified by 1H NMR,IR spectra and elemental analysis.Preliminary bioassay showed that all of them possessed some extent herbicidal activity against Brassica campestris and Echinochloa crusgalli.

【关键词】 哒嗪合成除草活性
【Key words】 pyridazinesynthesisherbicidal activity
【基金】 国家“973”计划(No.2003CB114400);国家自然科学青年基金(No.20302004)资助项目
  • 【文献出处】 有机化学 ,Chinese Journal of Organic Chemistry , 编辑部邮箱 ,2008年07期
  • 【分类号】TQ450.21
  • 【被引频次】12
  • 【下载频次】315
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