新型N-苯甲酰基硝基胍类化合物的合成及其杀菌活性

Synthesis and fungicidal activity of novel N-benzoyl nitroguanidine derivatives

为了得到具有较强杀菌活性的新型硝基胍化合物,以硝酸胍为起始原料,通过硝基化反应和取代反应,得到具有不同取代基的硝基胍化合物,再通过酰化反应,将硝基胍化合物与苯甲酰氯反应,得到6个未见文献报道的N-苯甲酰基硝基胍衍生物.目标化合物的结构通过核磁共振氢谱和质谱进行了表征,并采用平皿生长速率法对所合成的化合物进行了初步的杀菌活性测试,结果表明:在200μg/mL质量浓度下,化合物2b和2c对草坪褐斑菌的抑制活性分别为90.7%和87%,高于阳性对照恶霉灵.

To obtain the novel nitroguanidine derivatives with potent fungicidal activities,guanidine nitrate was used as the starting material.The substituted nitroguanidine compounds were given by the nitration and alkylation reactions with the guanidine nitrate.Six novel benzoyl nitroguanidine derivatives were designed and synthesized by the acylation reactions of benzoyl chloride with the substituted nitroguanidine compounds.The structures of the target molecules were characterized by nuclear magnetic resonance spectrum and mass spectrum.The preliminary fungicidal activities tests of the synthesized compounds were measured using plate growth rate method.The results show that inhibition rate of 2b and 2c at 200 μg/mL against Rhizoctonia solani AG-1-IB is 90.7％ and 87.0％,respectively;the activities of 2b and 2c are better than those of positive control hymexazol.