Enantioconvergent and Regioselective Deaminative Alkenylation of α‐Amino Acid Derivatives With Internal Alkynes

ABSTRACT

In this study, we disclose the first regio‐ and enantioselective deaminative alkenylation of amino acid derivatives with internal alkynes. This Ni‐catalyzed protocol provides direct access to chiral homoallylic carbonyl compounds from abundant amino acid building blocks and readily available alkynes. The transformation proceeds with excellent E / Z stereoselectivity and high levels of regio‐ and enantioselectivity, while accommodating a broad range of functional groups and both symmetrical and unsymmetrical internal alkynes. The synthetic utility of the method is demonstrated through the preparation and diversification of structurally complex molecules. Overall, this work establishes a general platform for enantioconvergent amino acid‐derived alkenylation and expands access to chiral homoallylic carbonyl frameworks from simple amino acid precursors.