Web Release Date: May 11,
Direct L-Proline-Catalyzed Asymmetric
-Amination of Ketones
gevig, and
rgensen*
Center for Catalysis, Department of Chemistry, Aarhus University, DK-8000 Aarhus C, Denmark
Received April 4, 2002

Abstract:
The first direct catalytic asymmetric
-amination of ketones catalyzed by L-proline has been developed. The reactions proceed with various azodicarboxylates as the nitrogen source in high yields and excellent enantioselectivities (up to 99% ee). The scope and potential of the reaction are demonstrated by further transformation of the
-hydrazino ketones formed to both optically active syn and anti-
-amino alcohol derivatives.
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