Copper-catalyzed Asymmetric Conjugate Addition to Challenging Michael Acceptors and Synthesis of Relevant Target Molecules

Abstract

We report herein the enantioselective Cu-catalyzed conjugate addition of organometallic reagents to sensitive Michael acceptors and their application to the synthesis of relevant target molecules. This is one of the most important methodologies to form a C–C bond in an enantioselective manner. A wide range of ?,?-unsaturated aldehydes and ?,?-unsaturated-?-ketoesters has been successfully used. Reactivity, regio- and enantioselectivities were strongly dependent on the reaction conditions, therefore moderate to very good results were obtained. Furthermore, ?-substituted-?-ketoesters were used as chiral building blocks for further derivatization with complete retention of the chiral information to obtain key compounds.