钯催化合成N-芳基-γ-胺基-γ-丁内酰胺类化合物  

Palladium Catalyzed Synthesis of N-Aryl-γ-amino-γ-lactams

作　　者：鲍峰玉[1] 刘兴源 张婉 李志 BAO Fengyu;LIU Xingyuan;ZHANG Wan;LI Zhi(College of Science,Henan Agricultural University,Zhengzhou 450002,China)

机构地区：[1]河南农业大学理学院,河南郑州450002

出　　处：《合成化学》2024年第8期705-710,共6页Chinese Journal of Synthetic Chemistry

摘　　要：γ-丁内酰胺是很多具有生物活性、药物活性化合物的核心结构单元。已报道的由过渡金属催化,直接合成N-芳基-γ-胺基-γ-丁内酰胺类化合物的反应,存在必须使用过氧化物、操作不便的局限性。以10%(物质的量分数,下同)Pd/C为催化剂,将芳香胺和N-甲基吡咯烷酮在空气气氛下的二甲苯中于100℃反应24 h得到N-芳基-γ-胺基-γ-丁内酰胺类化合物(3a~3g),产率高达91%。经过核磁氢谱、碳谱和高分辨质谱分析,产物的结构得到确证。Theγ-lactams are core structural units of a number of compounds with biological and medicinal activities.The reported reactions of transition metal-catalyzed direct synthesis of N-aryl-γ-amino-γ-lactams suffer from limitation of peroxides and operating inconvenience.10%(molar fraction,same below)Pd/C was used as catalyst.The reactions of aryl amines with N-methyl-2-pyrrolidone were conducted in xylene at 100℃ for 24 h in an air atmosphere and gave N-aryl-γ-amino-γ-lactam compounds(3a~3g)in up to 91% yield.The structures of the products were confirmed by 1 H NMR,13 C NMR and HR-MS(ESI)analysis.

关 键 词：钯 催化 合成 芳香胺 N-甲基吡咯烷酮 氧化胺化 γ-丁内酰胺 

分 类 号：O622.6[理学—有机化学]