N-[3-(4-喹唑啉基)氨基-1H-吡唑-4-甲酰基]醛腙类衍生物的合成及抗菌活性研究  

Synthesis and Fungicidal Activities of N-[(3-(4-Quinazolinyl)amino-1H-pyrazole-4-formyl)aldehyde Hydrazones

作　　者：高元磊[1] 林选福[1] 韩菲菲[1] 鲍小平[1] 

机构地区：[1]贵州大学精细化工针冗升发中心教育部绿色农药与农业生物工程重点实验室,贵阳550025

出　　处：《有机化学》2011年第10期1648-1652,共5页Chinese Journal of Organic Chemistry

基　　金：教育部科学技术研究重点(No.209110);贵州省农业攻关(No.20093010)资助项目

摘　　要：以4-氯喹唑啉、3-氨基-4-吡唑甲酸乙酯和芳醛为原料,合成了13个新型的N-[3-(4-喹唑啉基)氨基-1H-吡唑-4-甲酰基]醛腙类化合物,通过IR,1H NMR,13C NMR和元素分析对其结构进行了确认.初步生物活性测试结果表明,在50μg/mL浓度下,化合物5d对小麦赤霉菌和苹果腐烂菌的抑制率与对照药剂噁霉灵相当;化合物5k对小麦赤霉菌的抑制率则高于噁霉灵.Using 4-chloroquinazoline,ethyl 3-amino-4-pyrazolecarboxylate and aromatic aldehyde as starting compounds,thirteen novel N-[（3-（4-quinazolinyl）amino-1H-pyrazole-4-formyl]aldehyde hydrazones were synthesized.Their structures were confirmed by IR,1H NMR,13C NMR spectra and elemental analy-sis.Preliminary bioassay indicated that compound 5d exhibited similar antifungal activities against Gibber-ella zeae and Cytospora mandshurica at 50 μg/mL,compared with control agent（hymexazol）.In addition,compound 5k possessed higher inhibition rate against G.zeae than hymexazol.

关 键 词：喹唑啉 吡唑 酰腙 合成 抗菌活性 

分 类 号：TQ252[化学工程—有机化工] TQ450.1