Copper Catalyzed Enantioselective Alkylation of Pyrrole with β,-Unsaturated a-Ketoesters: Application to One-Pot Construction of the Seven-Membered Ring by Merging a Gold Catalysis.

A highly enantioselective Friedel-Crafts alkylation of pyrrole to β,-unsaturated a-ketoesters was developed by virtue of a chiral copper complex, affording the alkylated derivatives of pyrrole with good yields and excellent enantioselectivities. Moreover, merging copper catalysis with gold catalysis realized a one-pot construction of the seven-membered ring to give annulated pyrroles with moderate to good yields and high enantiomeric excesses. [ABSTRACT FROM AUTHOR]