新型腈基取代吡啶类化合物的合成  

Synthesis of Novel Cyanopyridine Derivatives

作　　者：陈识峰 CHEN Shi-feng(Zhejiang Yongning Pharmaceutical Co.,Ltd,Taizhou 318020,China)

机构地区：[1]浙江永宁药业股份有限公司,浙江台州318020

出　　处：《合成化学》2018年第1期15-21,共7页Chinese Journal of Synthetic Chemistry

基　　金：黄岩区重大科技计划项目(2004016)

摘　　要：以酰胺、醛、丙二腈和醋酸铵为主要原料,经氧化铝固载氟化钾催化反应合成了16个腈基取代吡啶类化合物(1a^1p),其中化合物1a^1o为新化合物,其结构经~1H NMR,^(13)C NMR和IR表征。对反应条件进行了优化。结果表明:在最佳反应条件[氧化铝固载氟化钾为催化剂,乙醇为溶剂,n(N-甲基吡咯烷酮)∶n(苯甲醛)∶n(醋酸铵)∶n(丙二腈)=1.0∶1.0∶1.5∶1.0,于80℃反应5 h]下,1a收率最高(91%)。Sixteen cyanopyridine derivatives(1a^1p)were synthesized by one-pot reaction catalyzed by KF-Al 2 O 3,using amide,aldehyde,malononitrile and ammonium acetate as the starting materials.Among them,1a^1o were new compounds.The structures were characterized by 1 H NMR,13 C NMR and IR.The reaction conditions were optimized.The results showed that 1a could be obtained with the highest yield(91%)under the optimum reaction conditions(KF-Al 2 O 3 as the catalyst,ethanol as the solvent,n(N-methyl pyrrolidone)∶n(benzaldehyde)∶n(ammonium acetate)∶n(malononitrile)=1.0∶1.0∶1.5∶1.0,reaction at 80℃for 5 h).

关 键 词：酰胺 醛 丙二腈 腈基取代吡啶类化合物 氧化铝固载氟化钾 催化 合成 

分 类 号：R978.1[医药卫生—药品] O621.3[医药卫生—药学]