Synthesis and Biological Activities of 4-Arylmethylidene-1-aryl-2-(selenomorpholin-4-yl)-2-imidazolin-5-one  

作　　者：胡利明 冯菊红 陈致远 刘钊杰 徐汉生 

机构地区：[1]Department of Chemistry,Xiamen University [2]Institute of Organic Synthesis,Central China Normal University [3]Department of Chemistry,Wuhan University

出　　处：《Chinese Journal of Chemistry》2003年第12期1642-1646,共5页中国化学（英文版）

摘　　要：In a search for novel agrochemical with high activity and low toxicity,a series of substituted 4,5 -dihydro-imidazol-5-one containing selenomorpholine group were synthesized by a three-step synthetic route starting from 2-azido-3-aryl-acrylic acid ethyl ester. The structures of title compounds were confirmed by 1H NMR ,IR,mass spectroscopy and elemental analysis. The preliminary bioassay against Gibberella zeae,Fusarium oxysporum,Pellicularia sasakii,Physalospora piricola and Cercospora beticola indicated that most title compounds displayed fungicidal activity at the concentration of 50 ppm and compounds 4l,4n,4o were found to have particularly high activities against Physalospora piricola. A further in vivo test showed that compounds 4l,4n and 4o possessed better fungicidal activity against Physalospora piricola at a concentration of 100 ppm than Carbendazim. To our knowledge,this is first report that 4,5 -dihydro-imidazol-5-one containing selenomorpholine group display fungicidal activity against Physalospora piricola.In a search for novel agrochemical with high activity and low toxicity,a series of substituted 4,5 -dihydro-imidazol-5-one containing selenomorpholine group were synthesized by a three-step synthetic route starting from 2-azido-3-aryl-acrylic acid ethyl ester. The structures of title compounds were confirmed by 1H NMR ,IR,mass spectroscopy and elemental analysis. The preliminary bioassay against Gibberella zeae,Fusarium oxysporum,Pellicularia sasakii,Physalospora piricola and Cercospora beticola indicated that most title compounds displayed fungicidal activity at the concentration of 50 ppm and compounds 4l,4n,4o were found to have particularly high activities against Physalospora piricola. A further in vivo test showed that compounds 4l,4n and 4o possessed better fungicidal activity against Physalospora piricola at a concentration of 100 ppm than Carbendazim. To our knowledge,this is first report that 4,5 -dihydro-imidazol-5-one containing selenomorpholine group display fungicidal activity against Physalospora piricola.

关 键 词：dihydro-imidazol-5-one selenomorpholine heterocyclic compound bioactivity 

分 类 号：O621[理学—有机化学]