新型2-取代苯甲酰基-5-烷基环戊酮的设计、合成与生物活性研究  

Design, Synthesis and Bioactivity of Novel 2-Aroyl-5-alkylcyclopentanone Derivatives

作　　者：徐海珍[1] 朱有全[2] 谢丽芬[2] 王晓芳[2] 

机构地区：[1]天津师范大学化学学院,天津300387 [2]南开大学元素有机化学国家重点实验室,天津300071

出　　处：《有机化学》2013年第1期143-147,共5页Chinese Journal of Organic Chemistry

基　　金：国家973计划(No.2010CB126103);国家自然科学基金(Nos.20772066;21072108);"十二五"科技支撑计划(No.2011BAE06B05-3)资助项目~~

摘　　要：为了发现具有良好生物活性的新型先导化合物,在综合多种高活性化合物结构特点的基础上,设计合成了一系列含苯甲酰基乙烯醇结构的2-取代苯甲酰基-5-烷基-环戊酮类化合物.以己二酸二乙酯为原料,经6步反应制得目标产物,其结构经IR,1H NMR,X射线及元素分析或高分辨质谱确证,并对该类化合物合成方法进行了探讨.初步生测结果表明,部分化合物对油菜表现出明显的抑制活性,在100μg/mL浓度下对油菜的抑制率达到60%以上.To find new lead compounds with muti-bioactivities, a series of novel 2-aroyl-5-alkylcyclopentanone derivatives containing 2-bezoylenthenol were designed on the base of various commercial products. The target compounds were synthe- sized from diethyl adipate in 6 steps. Their structures were confirmed by IR, 1H NMR spectra, X-ray and elemental analysis or HRMS. The preliminary bioassay results indicated that some compounds showed obvious inhibition effects against Brassica campestris, and the herbicidal activities were more than 60% at 100 μg/mL.

关 键 词：对羟基苯基丙酮酸双氧化酶 芳酰基乙烯醇 环戊酮 除草活性 

分 类 号：TQ457.2[化学工程—农药化工]