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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%。
With the methyl ketone, diethyl oxalate or dimethyl oxalate, hydroxylamine hydrochloride and hydrazine hydrate as raw materials, by condensation, cyclization, hydrolysis and other reactions, the substituted pyrazole ring, isoconazole ring into the benzimidazole 2 , 13 novel 2-substituted benzimidazoles derivatives were designed and synthesized. Their structures were confirmed by IR, ESI-MS and 1H-NMR. The preliminary bioassay results showed that all the target compounds exhibited antibacterial activity against six tested pathogens at a concentration of 100 mg / L. Among them, 2-pyrazole-substituted compounds 2a ~ 2d inhibited the growth of Glomerella cingulata The inhibitory rate was over 80%. The inhibitory rate of 2-isosulfazole substituted compound 4a on Alternaria solani, apple anthracnose and Magnaport hegrisease was 100%.