Achim Link
Yujing Zhou
Stephen L. Buchwald

CuH-Catalyzed Asymmetric Reductive Amidation of α,β-Unsaturated Carboxylic Acids

“,
Org. Lett.
,
2020
,
22
(
14
)
,
5666-5670
.
ol0c02064_0007
Abstract

The direct enantioselective copper hydride (CuH)-catalyzed synthesis of β-chiral amides from α,β-unsaturated carboxylic acids and secondary amines under mild reaction conditions is reported. The method utilizes readily accessible carboxylic acids and tolerates a variety of functional groups in the β-position including several heteroarenes. A subsequent iridium-catalyzed reduction to γ-chiral amines can be performed in the same flask without purification of the intermediate amides.