取代苯肼类化合物的设计、合成及杀菌活性  

Design,synthesis and fungicidal activity of substituted phenylhydrazines

作　　者：李慧超 杨吉春 孙芹 兰杰 关爱莹 LI Huichao;YANG Jichun;SUN Qin;LAN Jie;GUAN Aiying(National Engineering Research Center of Pesticide,State Key Laboratory of the Discovery and Development of Novel Pesticide,Shenyang Sinochem Agrochemicals R&D Co.,Ltd.,Shenyang 110021,China)

机构地区：[1]沈阳中化农药化工研发有限公司新农药创制与开发国家重点实验室,农药国家工程研究中心,沈阳110021

出　　处：《农药》2024年第10期712-716,727,共6页Agrochemicals

摘　　要：[目的]寻找结构相对简单且具有较好杀菌活性的新化合物。[方法]利用中间体衍生化法,将具有广谱杀菌活性的二苯胺类化合物中的氨基用联氨基替换,通过设计、合成、筛选及结构优化,得到15个新型取代苯肼类化合物。[结果]在25 mg/L剂量下,化合物3c、4a、4b、4c、6a、6b对黄瓜霜霉病的防效均不低于80%;在0.9 mg/L剂量下,化合物6b对黄瓜灰霉病菌的抑制率为100%,与同等剂量下的氟啶胺相当。[结论]化合物6b具有较好的杀菌活性,可作为先导化合物进一步研究。[Aims]The aim of this study is to explore new fungicidal compounds with relatively simple structures.[Methods]Basing on Intermediate Derivatization Method,we used hydrazineyl to replace amino of diphenylamines which were known for their broad-spectrum fungicidal activity.Through design,synthesis,screening and structural optimization,we obtained 15 novel substituted phenylhydrazine compounds.[Results]At the concentration of 25 mg/L,compounds 3c,4a,4b,4c,6a and 6b showed a control effect of no less than 80%against cucumber downy mildew.At 0.9 mg/L,compound 6b had a 100%inhibition rate against Botrytis cinerea,equivalent to fluazinam at the same dose.[Conclusions]Compound 6b has good fungicidal activity and can be further studied as a lead compound.

关 键 词：中间体衍生化法 取代苯肼类化合物 合成 杀菌活性 

分 类 号：TQ450.11[化学工程—农药化工]