樟脑酸基双酰肼化合物的合成及其抑菌活性  

Synthesis and Antifungal Activity of Camphoric Acid-Based Diacylhydrazine Compounds

作　　者：马献力[1,2] 李芳耀[1,2] 段文贵[1] 林桂汕[1] 陈乃源[1] 马媛[1] 

机构地区：[1]广西大学化学化工学院,广西南宁530004 [2]桂林医学院药学院,广西桂林541004

出　　处：《精细化工》2015年第12期1426-1430,共5页Fine Chemicals

基　　金：国家自然科学基金项目(31260164);广西高校科学技术研究重点项目(ZD2014098)~~

摘　　要：以樟脑酸为原料,经过脱水反应制备樟脑酸酐,再与芳酰肼发生N-酰化反应,合成得到10个樟脑酸基双酰肼化合物Ⅲa~Ⅲj。初步探索了合成条件,并利用FTIR、1HNMR、13CNMR和ESI-MS对目标产物进行结构表征。初步的生物活性测试表明,在50 mg/L质量浓度下,部分化合物表现出良好的抑菌活性,其中樟脑酸基烟酰肼Ⅲh对苹果轮纹病菌的抑制率高达96.3%,优于阳性对照嘧菌酯。Camphorlc anhydride was prepared by using camphoric acid as raw materials. Then, ten novel camphoric acid-based diacylhydrazine compounds Ⅲ a ～Ⅲj were synthesized by the N-acylation reaction of camphoric anhydride with aromatic acylhydrazines. The synthetic conditions were investigated preliminarily and the target compounds were characterized by FTIR, 1HNMR, 13 CNMR and ESI-MS. The preliminary bioassay showed that, with the concentration of 50 mg/L, part of the title compounds exhibited good antifungal activity, in which compound camphoric acid-based nicotinoyl hydrazine Ⅲ h had inhibition ratio of 96.3% against Physalospora piricola （better than that of the positive control azoxystrobin）.

关 键 词：樟脑酸 双酰肼 抑菌活性 精细化工中间体 

分 类 号：TQ351[化学工程]