Organocatalytic Enantioselective Multicomponent Synthesis of Pyrrolopiperazines

The first organocatalytic multicomponent synthesis of enantioenriched pyrrolopiperazines is reported. These biologically relevant fused tricyclic products were obtained under catalytic iminium activation through a reaction sequence involving an enantioselective Michael addition followed by an iminium ion trapping via Pictet–Spengler cyclization (MAPS sequence). Substantial possibilities for variation on the three reaction partners [β‐keto ester, enal and N ‐(2‐aminoethyl)pyrrole] along with excellent enantioselectivities are the highlights of the present transformation.