Lewis Acid and (Hypo)iodite Relay Catalysis Allows a Strategy for the Synthesis of Polysubstituted Azetidines and Tetrahydroquinolines.

A catalytic [3 + 1]-annulation reaction between cyclopropane 1,1-diester and aromatic amine is developed based on the relay catalysis strategy. Lewis acid-catalyzed nucleophilic ring opening of cyclopropane 1,1-diester with aromatic amine and (hypo)iodite-catalyzed C-N bond formation are combined successfully in one reaction. Using this reaction, biologically important azetidines and tetrahydroquinolines can be prepared directly.