Lewis Acid Catalyzed Annulation of Donor-Acceptor Cyclopropane and N-Tosylaziridinedicarboxylate: One-Step Synthesis of Functionalized 2H-Furo[2,3-c]pyrroles

An efficient MgI2-catalyzed annulation between donor-acceptor cyclopropane and N-tosylaziridinedicarboxylate to access highly substituted 2H-furo[2,3-c]pyrrole bearing two rings and four stereocenters, including one quaternary carbon stereocenter, has been developed. This methodology can be used for the synthesis of biologically active compounds like IKM-159. This work also offers an insight into the mechanism of the annulation process.