Direct Synthesis of α-Amino Acid Derivatives by Hydrative Amination of Alkynes.

α-Amino acid derivatives are key components of the molecules of life. The synthesis of α-amino carbonyl/carboxyl compounds is a contemporary challenge in organic synthesis. Herein, we report a practical method for the preparation of α-amino acid derivatives via direct hydrative amination of activated alkynes under mild conditions, relying on sulfinamides as the nitrogen source. Computational studies suggest that the reaction is enabled by a new type of sulfonium [2,3]-sigmatropic rearrangement.
(© 2022 The Authors. Angewandte Chemie International Edition published by Wiley-VCH GmbH.)