Tebufloquin的合成与生物活性  

Synthesis and Biological Activity of Tebufloquin

作　　者：郝树林[1] 田俊峰[1] 徐英[1] 范文玉[2] 姜艾汝[1,2] 刘长令[1] 

机构地区：[1]沈阳化工研究院有限公司新农药创制与开发国家重点实验室,沈阳110021 [2]沈阳化工大学,沈阳110142

出　　处：《农药》2012年第6期410-412,共3页Agrochemicals

基　　金：国家重点基础研究发展规划项目(973项目:2010CB126105;2010CB735601;2012CB724501);国家"十二.五"科技支撑计划项目(2011BAE06B00;2011BAE06B01;2011BAE06B02;2011BAE06B03;2011BAE06B05)

摘　　要：[目的]Tebufloquin是一类作用机制新颖的杀菌剂,与现有杀菌剂无交互抗性,探索了其合成方法并进行了生物活性测定。[结果]以邻氟苯胺为原料,经5步反应合成了目标化合物tebufloquin,经核磁、质谱验证了其结构,生测结果表明该化合物具有广谱的杀菌活性,尤其对水稻稻瘟病有特效。[结论]Tebufloquin具有优异的杀菌活性,值得大家重视,同时该合成方法对工业化生产也具有一定的指导意义。[Aims] Tebufloquin is a new fungicide with novel mode of action and has no cross resistance with other existing fungicides, so the synthetic method was explored and bioassay activity was evaluated. Compared to the known synthetic methods, a better way was selected. [Results] Tebufloquin was＇prepared from 2-fluoroaniline as a starting material through five steps and its chemical structure was confirmed by ~H NMR and LC-MS. The bioassay showed that tebufloquin has a broad spectrum of fungicidal activity, especially against rice blast. [Conclusions] Tebufloquin, a kind of novel fungicide, is worthy of our attention and this synthetic method provides certain directive significatice for industrial production.

关 键 词：tebufloquin 杀菌剂 合成 水稻稻瘟病 

分 类 号：TQ450.21[化学工程—农药化工]