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.