1-取代苯胺基-4,4-二甲基-2-(1H-1,2,4-三唑-1-基)-1-戊烯-3-酮的合成及其生物活性  

Synthesis and Bioactivity of 1-Substitutedanilino-4,4-dimethyl-2-(1H-1,2,4-triazol-1-yl)-1-penten-3-one

作　　者：于海波[1] 郭湘云[1] 汪清民[1] 陈莉[1] 成俊然[1] 黄润秋[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：《农药学学报》2005年第2期109-113,共5页Chinese Journal of Pesticide Science

摘　　要：为寻找高活性的烯基三唑类杀菌剂,利用1-二甲氨基-4,4-二甲基2(1H-1,2,4-三唑-1-基)-1-戊烯-3-酮与取代苯胺进行亲核取代反应,合成了一系列新型1-取代苯胺基-4,4-二甲基-2-(1H-1,2,4-三唑-1-基)-1-戊烯-3-酮化合物,其结构经元素分析、核磁共振氢谱确认。由1HNMR分析结果推测该类化合物E式构型为优势产物。初步生物活性测试结果表明,化合物1n(取代基R=3OCH3)在50μg/mL浓度下对葡萄白腐菌Coniothyrium diplodiella、黄瓜黑星菌Cladosporium cucumerinum等的抑制率均达到100%;在10μg/mL浓度下对促进黄瓜子叶生根的活性达到155.2%。In order to search for the active alkenyl triazole fungicide, a series of novel 1-substituted anilino-4,4-dimethyl-2-(1H-1,2,4-triazol-1-yl)-1-penten-3-ones were synthesized with good yields by the nucleophilic reaction of substituting anilines with 1-(N,N-dimethylamino-)-[KG*5]4,4-dimethyl-2-(1H-(1,2,4-)triazol-1-yl)-1-penten-3-one. Their structure were confirmed by elemental analysis and (()^(1)H NMR). The result of ()^(1)H NMR showed that E-configuration were predominant products. The (preliminary) biological tests indicated that the relative inhibition rate of compound 1n(R=3-OCH_3) to Coniothyrium diplodiella and (Cladosporium) (cucumerinum) were all 100% at the concentration of (50 μg/mL), and its relative promote to (cucumber) root is 155.2%.

关 键 词：苯胺 亲核取代 1H-1 2 4-三唑 生物活性 

分 类 号：O621[理学—有机化学] O626.42[理学—化学]