Enantioselective Copper‐Catalyzed Azide–Alkyne Click Cycloaddition to Desymmetrization of Maleimide‐Based Bis(alkynes)

Abstract

A copper catalyst system derived from TaoPhos and CuF2 was used successfully for catalytic asymmetric Huisgen [3+2] cycloaddition of azides and alkynes to give optically pure products containing succinimide- and triazole-substituted quaternary carbon stereogenic centers. The desired products were obtained in good yields (60-80 %) and 85:15 to >99:1 enantiomeric ratio (e.r.) in this click cycloaddition reaction.