Abstract
Comprehensive SummaryAn efficient method for asymmetric synthesis of acyclic α‐tertiary amine derivatives has been achieved through enantioselective aminations of α‐branched ynones with azodicarboxylates enabled by chiral phosphoric acid catalysis. Moreover, kinetic resolution of racemic starting material was realized under these conditions, which gave access to valuable enantioenriched α‐substituted ketones. A wide array of α‐aryl and alkyl‐substitutions, and the substituted alkynyl groups were well compatible with this method, producing both the amination products and the recovered ketones with good to high enantioselectivities.
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