Copper-catalyzed synthesis of aziridines

Abstract This chapter provides a general outlook on the developments in the copper-catalyzed aziridination reaction for the synthesis of the smallest nitrogen-containing heterocycle, aziridine. In the last few decades, several methodologies have been applied in the transition-metal catalyzed aziridination reaction, and, without a doubt, the copper-catalyzed nitrene transfer to olefins is the most widely applied method for the preparation of these heterocycles. This obviously demonstrates that these protocols provide a very important tool in organic synthesis, attracting significant interest due to the potential use of aziridines as intermediates in the preparation of more complex molecules.