利用aza-Michael/Michael串联环化反应合成螺巴比妥哌啶酮衍生物  

Synthesis of Spirobarbiturate Piperidin-2-one Derivatives via Cascade Aza-Michael/Michael Cyclization Reaction

作　　者：刘雪华 王川川 王新璐 马志伟 孟蕾 丁德刚 刘俊桃 陈亚静 Liu Xuehua;Wang Chuanchuan;Wang Xinlu;Ma Zhiwei;Meng Lei;Ding Degang;Liu Juntao;Chen Yajing(School of Pharmaceutical Sciences,Zhengzhou University,Zhengzhou 450001;Faculty of Science,Henan University of Animal Husbandry and Economy,Zhengzhou 450046;Henan Institute of Veterinary Drug and Feed Control,Zhengzhou 450008)

机构地区：[1]郑州大学药学院,郑州450001 [2]河南牧业经济学院理学部,郑州450046 [3]河南省兽药饲料监察所,郑州450008

出　　处：《有机化学》2021年第11期4450-4458,共9页Chinese Journal of Organic Chemistry

基　　金：河南省重点研发与推广专项(科技攻关)(Nos.202102110067,212102110439);河南省自然科学基金(Nos.202300410188,212300410152);河南牧业经济学院(Nos.2019HNUAHEDF011,XKYCXJJ2020006)资助项目.

摘　　要：发展了巴比妥衍生烯烃化合物与N-烷氧基丙烯酰胺之间的串联aza-Michael/分子内Michael加成反应.该反应条件温和,适用于克级制备,为具有生物活性的螺巴比妥分子的高效合成提供了一种实用的方法.A highly efficient cascade aza-Michael/intramolecular-Michael reaction employing barbiturate-derived alkenes and N-alkoxy acrylamides has been developed.The reaction proceeds smoothly under mild conditions and is amenable to gram scale synthesis,providing a practical tool in the synthesis of bioactive spirobarbiturate piperidin-2-ones molecules in moderate to good yields.

关 键 词：螺巴比妥 哌啶酮 串联反应 MICHAEL加成 

分 类 号：TQ460.1[化学工程—制药化工] O626[理学—有机化学]