Highly Efficient Synthesis of β-Amino Acid Derivatives via Asymmetric Hydrogenation of Unprotected EnaminesClick to copy article linkArticle link copied!
- 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
Abstract
A direct asymmetric hydrogenation of unprotected enamino esters and amides is described. Catalyzed by Rh complexes with Josiphos-type chiral ligands, this method gives β-amino esters and amides in high yield and high ee (93−97% ee). No acyl protection/deprotection is required.
*
In papers with more than one author, the asterisk indicates the name of the author to whom inquiries about the paper should be addressed.
†
Department of Process Research, Merck and Co., Inc.
‡
Department of Analytical Research, Merck and Co., Inc.
§
Solvias AG.
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