Asymmetric Michael Addition of Malonates to Enones Catalyzed by a Primary beta-Amino Acid and Its Lithium Salt

[摘要]：Highly enantioselective Michael addition of malonates to enones was achieved using a mixed catalyst consisting of a primary beta-amino acid, O-TBDPS (S)-beta-homoserine, and its lithium salt. Various cyclic and acyclic enones were converted into 1,5-ketoesters in high yields (up to 92%) with high enantioselectivity (up to 97% ee) under mild reaction conditions. Details of synthesis of the catalyst, optimization of the reaction conditions for the Michael addition reaction, and a plausible reaction mechanism are described.

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