摘要
以甲基酮、草酸二乙酯或草酸二甲酯、盐酸羟胺和水合肼为原料,通过缩合、环合、水解等反应,将取代吡唑环、异唑环引入苯并咪唑的2位,设计合成了13个未见文献报道的2-取代苯并咪唑类衍生物,其结构经红外、电喷雾串联质谱(ESI-MS)和核磁共振氢谱确证。初步生物活性测试结果表明,在100 mg/L质量浓度下,所有目标化合物对6种供试病原菌均具有一定的抑菌活性,其中2-吡唑取代的化合物2a～2d对苹果炭疽病菌Glomerella cingulata的抑制率在80%以上,2-异唑取代的化合物4a对番茄早疫病菌Alternaria solani、苹果炭疽病菌和水稻稻瘟病菌Magnaport hegrisease的抑制率达100%。
Thirteen 2-heterocyclic-benzimidazole derivatives were synthesized from methyl ketone,diethyl oxalate or dimethyl oxalate,hydroxylamine hydrochloride,hydrazine hydrate as starting materials via several reactions including condensation,cyclization and hydrolysis.The structures of all compounds were confirmed by IR,ESI-MS and 1H NMR.Preliminary bioassay showed that all the compounds exhibit some fungicidal activity against six fungi tested at the concentration of 100 mg/L,among them,the inhibition rate of 2a-2d against Glomerella cingulata were above 80%,4a showed 100% inhibition rate against Alternaria solani,G.cingulata and Magnaport hegrisease.
出处
《农药学学报》
CAS
CSCD
北大核心
2011年第5期448-452,共5页
Chinese Journal of Pesticide Science
关键词
苯并咪唑
合成
抑菌活性
benzimidazoles
synthesis
fungicidal activity
