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

作　　者：赵建[1] 宁君[1] 蒋志福[1] 高贝贝[1] 袁会珠[1] 折冬梅[1] 

机构地区：[1]中国农业科学院植物保护研究所农业部作物有害生物综合治理重点实验室,北京100193

出　　处：《合成化学》2012年第5期582-585,590,共5页Chinese Journal of Synthetic Chemistry

基　　金："十一.五"国家科技支撑计划资助项目(2009BAK61B04);公益性行业(农业)科技专项资助项目(200903054)

摘　　要：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.

关 键 词：L-缬氨酸 混合酸酐法 合成 抑菌活性 

分 类 号：O625.63[理学—有机化学]