【作者】 王闽龙； 芮朋； 纪明山； 祁之秋； 李兴海；

【Author】 WANG Minlong;RUI Peng;JI Mingshan;QI Zhiqiu;LI Xinghai;College of Plant Protection,Shenyang Agricultural University;

【机构】 沈阳农业大学植物保护学院；

【摘要】 [目的]为了获得具有高效杀菌活性的先导化合物,探索合成了结构新颖的的2-取代苯基-2-氧代乙磺酰胺衍生物。[方法]以取代苯乙酮为原料经过磺化、氯化反应,制备2-取代苯基-2-氧代乙磺酰氯,再与2-三氟甲基-4-氯苯胺反应,制备Ⅳ-（2-三氟甲基-4-氯苯基）-2-取代苯基-2-氧代乙磺酰胺化合物（ⅡI）。再以采自辽宁省多个地区灰霉病病菌为供试靶标,采用菌丝生长速率法和活体盆栽试验对化合物进行活性筛选。[结果]合成了17个2-取代苯基-2-氧代酰氧基乙磺酰胺衍生物,结构经¹H NMR,GC-MS及IR确认。生测表明:化合物Ⅲ-3对灰霉病病菌DD-15和SY-10的EC₅₀为2.27μg/mL和1.94μg/mL,且对采自辽宁省各地区的多个灰霉病病菌与其他6种病原菌也具有非常高的杀菌活性。[结论]:该类化合物具有很好的杀菌效果,有进一步开发的价值。更多还原

【Abstract】 [Objective]To explore the novel structure compounds with high fungicidal activity,a series of novel 2-substituted phenyl-2-oxoethylsulfonamides were synthesized.[methods]2-substituted phenyl-2-oxoethylsulfochloride,prepared from readily available substitutedacetophenone,were allowed to react with2-amino-5-chlorobenzotrifIuorideto give the correspondingN-(2-trifluoromethyl-4-chlorophenyl)-2-substituted phenyl-2-oxoethylsulfonamides.The fungicidal activities againstBotrytis cinerea Pers.strains collected from different areas in Liaoning,China in vitro were evaluated by adopting mycelium growth rate method,which in vivo by houseplants method,[result]172-substituted phenyl-2-oxoethylsulfonamides,whose structures were confirmed by IR,~1H NMR and GC-MS,had been synthesized.The results of the bioassay showed that the compounds Ⅲ-3 possessed excellent fungicidal activity against Botrytis cinereaDD-15 and SY-10,the EC50 values of which were 2.27 and 1.94 μg/mL,respectively.The further bioassay showed that the compounds III has good fungicidal activities against not only B.cinerea but also such 6 pathogenic bacteria as Pyriculariagrisea.[Conclusion]All the compounds show high fungicidal activities and can be used as possible new lead compounds for further developing novel fungicides against B.cinerea.更多还原