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Highly Efficient Synthesis of β-Amino Acid Derivatives via Asymmetric Hydrogenation of Unprotected Enamines

2004; American Chemical Society; Volume: 126; Issue: 32 Linguagem: Inglês

10.1021/ja047901i

1943-2984

Yi Hsiao, Nelo R. Rivera, Thorsten Rosner, Shane W. Krska, Eugenia Njolito, Fang Wang, Yongkui Sun, Joseph D. Armstrong, Edward J. J. Grabowski, Richard D. Tillyer, Felix Spindler, Christophe Malan,

Asymmetric Synthesis and Catalysis

A direct asymmetric hydrogenation of unprotected enamino esters and amides is described. Catalyzed by Rh complexes with Josiphos-type chiral ligands, this method gives beta-amino esters and amides in high yield and high ee (93-97% ee). No acyl protection/deprotection is required.