新型N-苯乙酰缬氨酰胺衍生物的“一锅法”合成及其抑菌活性

“One-pot” Synthesis and Inhibitory Activities of Novel N-phenylacetyl-L-valinamide Derivatives

以L-缬氨酸为起始原料,三乙胺为酰化剂,在液-液两相反应体系中通过混合酸酐法"一锅"合成了7个未见文献报道的缬氨酰胺类衍生物(5a～5g),其结构经1H NMR,IR和HR-MS表征。应用生长速率法对其生物活性进行了初步测试,结果表明,5对卵菌纲疫霉属病菌有一定的抑菌活性,其中5e在给药量为50 mg.L-1时,对黄瓜疫霉病菌的抑制率达49.2%。

Seven novel valinamide derivatives（5a～5g） were synthesized from L-valine by mixed anhydride method in liquid-liquid biphasic system using triethylamine as the acylating regent in ＂one-pot＂.The structures were confirmed by 1H NMR,IR and HR-MS.Preliminary biological tests by the method of mycelial growth rate in vitro indicated that some of these compounds exhibited inhibitory activity against Phytophthora spp at 50 mg·L-1,especially,5e showed 49.2% inhibitory activity against Phytophthora melonis.