2-酰基-氰基乙酸衍生物的合成及生物活性  

Synthesis and Bioactivity of 2-Aceto-cyanoacetic Acid Derivatives

作　　者：李洋[1,2] 张志国[2,3] 迟会伟 罗艳梅[2] 刘长令[2] 李正名[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 [2]沈阳化工研究院,沈阳110021 [3]沈阳化工学院化学系,沈阳110142

出　　处：《高等学校化学学报》2010年第9期1798-1804,共7页Chemical Journal of Chinese Universities

基　　金：国家"十一五"科技支撑项目(批准号:2006BAE01A01-2)资助

摘　　要：设计并合成了21个新型2-酰基-氰基乙酸类化合物,应用氢核磁共振谱、元素分析和红外光谱验证了它们的结构,并测试了其生物活性.部分化合物对朱砂叶螨(Tetranychus cinnabarinus)具有活性,化合物4e和4k在600mg/L浓度下呈现100%的杀螨活性;部分化合物具有一定杀菌和除草活性,化合物4k和4s在400mg/L浓度下对小麦白粉病(Blumeria graminis)的抑制率达到100%,化合物4m在1000mg/L浓度下可以很好地防治苘麻(Abutilon theophrasti).初步探讨了化合物结构与生物活性关系.For finding excellent acaricide,a series of novel 2-acyl-cyanoacetic acid derivatives was designed and synthesized based on cyflumetofen. Their structures were confirmed by 1H NMR,IR and elemental analysis. Preliminary biological evaluation showed that several compounds had acaricidal activity,with compounds 4e and 4k having 100% control against Tetranychus cinnabarinus at 600 mg/L. Some compounds exhibited fungicidal activity and herbicidal activity,compounds 4k and 4s could completely control against Blumeria graminis at 400 mg/L,compound 4m had good control of Abutilon theophrasti at 1000 mg/L. The relationship between the structures and the biological activity was also discussed.

关 键 词：2-酰基氰基乙酸衍生物 杀螨活性 杀菌活性 除草活性 

分 类 号：O626[理学—有机化学]