Enantioselective Synthesis of Chiral Pyrrolidine-Fused Piperazine Derivatives via Diaza-Cope Rearrangement

Abstract

Piperazinopyrrolidine and pyrrolidinone derivatives represent one important class of natural products and pharmaceutical agents, which often display interesting biological activities. In this study, a highly efficient synthetic method was developed for the construction of enantiomerically pure chiral piperazinopyrrolidine derivatives via diaza-Cope rearrangement (DCR). This protocol can provide a new approach for the asymetric syntheses of some biologically relevant products possessing piperazinopyrrolidine moiety.