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由1-芳基-3,5-二甲基吡唑-4-羧酸与适当的有机锡反应,合成表征了一系列的1-芳基-3,5-二甲基吡唑-4-羧酸有机锡酯(1～14),并通过单晶衍射确定了1-苯基-3,5-二甲基吡唑-4-羧酸三乙基锡酯(7)的结构。该化合物与一分子水共同结晶,通过分子间O-H…O及O-H…N氢键形成二维网状结构。杀菌活性筛选表明新合成的化合物对于番茄早疫菌、花生褐斑菌、小麦赤霉菌、苹果轮纹菌及灰霉菌全部具有良好的生长抑制作用。1-苯基-3,5-二甲基吡唑-4-羧酸三乙基锡酯及1-(2-吡啶基)-3,5-二甲基吡唑-4-羧酸三乙基锡酯在50μg.mL-1浓度下的体外实验中表现出很高的生长抑制率。对于高活性的三取代锡羧酸酯进行了EC50值的测定,结果表明1-(2-吡啶基)-3,5-二甲基吡唑-4-羧酸三乙基锡酯对苹果轮纹菌的EC50值为0.06μg.mL-1,对小麦赤霉菌的EC50值为0.14μg.mL-1。
From 1-aryl-3,5-dimethylpyrazole-4-carboxylic acid with a suitable organotin, a series of 1-aryl-3,5-dimethylpyrazol-4- (1-14) carboxylic acid and the structure of triethyl tin ester (7) of 1-phenyl-3,5-dimethylpyrazole-4-carboxylic acid was confirmed by single crystal diffraction. The compound co-crystallizes with one molecule of water and forms a two-dimensional network structure through intermolecular O-H ... O and O-H ... N hydrogen bonds. Screening of the bactericidal activity showed that the newly synthesized compounds all had good growth inhibitory effects on A. solani, P. peanut, G. graminearum, C. rubrum and Botrytis cinerea. Triethyl tin 1-phenyl-3,5-dimethylpyrazole-4-carboxylate and triethyl 1- (2-pyridyl) -3,5-dimethylpyrazole- The base tin ester showed a high growth inhibition rate in in vitro experiments at a concentration of 50 μg.mL-1. EC50 values were measured for the highly active tri-substituted tin carboxylates. The results showed that the EC50 value of 1- (2-pyridyl) -3,5-dimethylpyrazole-4- The EC50 value of the fungi was 0.06 μg.mL-1, and the EC50 value of the Gibberella zeae was 0.14 μg.mL-1.