A Facile Cu(I)/BINAP-Catalyzed Asymmetric Approach to Functionalized Pyroglutamate Derivatives Bearing a Unique Quaternary Stereogenic Center

A direct and facile access to enantioenriched pyroglutamate derivatives bearing a unique quaternary stereogenic center has been developed via Cu(I)/BINAP-catalyzed tandem Michael addition–elimination of α-substituted aldimino esters with Morita–Baylis–Hillman (MBH) carbonates followed by a deprotection/lactamization protocol, which performs well over a broad scope of substrates and provides biologically active pyroglutamate derivatives in good yields and excellent enantioselectivities.