Ag_(2)O/PPh_(3)催化合成4-位季碳吡咯烷衍生物

Synthesis of C4-quaternary Pyrrolidine Derivatives Catalyzed by Ag_(2)O/PPh_(3)

本文报道了以Ag_(2)O/PPh_(3)为催化体系,催化偶氮甲碱叶立德与a-取代的丙烯酰胺之间的1,3-偶极环加成反应构建4-位季碳的吡咯烷衍生物。通过条件优化和底物适应性研究,以大于20︰1的非对映选择性及87%~97%的产率合成了7个4-位季碳吡咯烷类化合物,并且该反应条件温和,催化剂廉价易得。

This paper reports the 1,3-dipolar cycloaddition reaction of azomethine ylides witha-substituted acrylamide to form pyrrolidine derivatives containing a C4-quaternary center using Ag_(2)O/PPh_(3) as catalyst system.Through the optimization of reaction conditions and the study of substrate adaptability,seven pyrrolidine derivatives containing a C4-quaternary center were synthesized with more than 20︰1 diastereoselectivity and 87%~97%yields.The reaction conditions were mild and the catalysts were cheap and available..