Catalytic Asymmetric Bromination and Chlorination of β‐Ketoesters

Abstract
The first general catalytic asymmetric bromination and chlorination of β-ketoesters has been developed. The reactions proceed for both acyclic and cyclic β-ketoesters catalyzed by chiral bisoxazolinecopper(II) complexes giving the corresponding optically active α-bromo- and α-chloro-β-ketoesters in high yields and moderate to good enantioselectivities. For the optically active chlorinated products the isolated yields are in the range of 88–99 % and the enantiomeric excesses up to 77 % ee, while the optically active brominated adducts are formed in 70–99 % isolated yield and up to 82 % ee. Based on the absolute configuration of the optically active products, the face selectivity for the catalytic enantioselective halogenation is discussed based on a bidentate coordination of the β-ketoester to the chiral catalyst and a X-ray structure of chiral α,γ-diketoesterenolatebisoxazolinecopper(II) complex.