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以环十二酮为原料合成α-取代环十二酮和α-取代环十二二酮,再与2,4-咪唑啉二酮膦酸酯和2-硫代-2,4-咪唑啉二酮分别发生Wittig-Horner反应和Knoevenagel缩合反应,合成了一系列目标化合物,它们的化学结构通过IR,1H NMR,13C NMR和元素分析进行了表征.初步生物活性测试结果表明,部分化合物10,11A,11B,12A,12B,13A,14B和16在50μg/mL浓度时对芦笋茎枯、茄绵疫以及油菜菌核病菌均有优良的抑制活性,抑制率在70%~98%之间,进一步的生物测试结果表明,化合物12B,13A和14B对芦笋茎枯的EC50值分别为15.80,31.34和44.26μg/mL.
Α-Substituted cyclododecanone and α-Substituted cyclododecanone were synthesized from cyclododecanone and reacted with 2,4-imidazolidinedione phosphonate and 2-thio-2,4-imidazoline Diketones were subjected to Wittig-Horner reaction and Knoevenagel condensation reaction respectively to synthesize a series of target compounds whose chemical structures were characterized by IR, 1H NMR, 13C NMR and elemental analysis.The preliminary bioassay results showed that some compounds 10, 11A, 11B, 12A, 12B, 13A, 14B and 16 had excellent inhibitory activity against Asparagus officinalis, Eggplant disease and Sclerotinia sclerotiorum at the concentration of 50μg / mL with the inhibitory rate between 70% and 98% Further bioassay results showed that the EC50 values of compound 12B, 13A and 14B to Asparagus stem flesh were 15.80, 31.34 and 44.26μg / mL, respectively.