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

作　　者：胡方中[1] 张桂峰[1] 邹小毛[1] 刘斌[1] 朱有全[1] 杨华铮[1] 

机构地区：[1]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,天津300071

出　　处：《有机化学》2008年第7期1227-1232,共6页Chinese Journal of Organic Chemistry

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

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.A series of novel 3-（substituted benzyloxy）-6-[（un）substituted 1H-pyrazol-l-yl]pyridazine derivatives 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 

分 类 号：TQ450.21[化学工程—农药化工]