Synthesis of α-Amino Acid Amides: Ruthenium-Catalyzed Animation of α-Hydroxy Amides

摘要

α-Amino acid amides represent an interesting subclass of amino acid derivatives. In general, such compounds are biologically active and possess therapeutically useful properties. Selected examples of such compounds are: 1, which is used for the treatment of metabolic syndrome, potent inhibitors for 11-3-hydroxysteroid dehydrogenase 1 (2), and top-selling drugs such as Lidoderm (3), Vyvanse (4), Altace (5), and Cefprozil (6; Scheme 1). Additionally, α-amino acid amides serve as synthetically useful intermediates for organic synthesis as well as organocatalysts and bidentate ligands for stereoselective transformations.