Efficient synthesis of protected β-amino acid derivatives via asymmetric hydrogenation

ORGN 666

Qian Dai and Weiran Yang. Department of Chemistry, The Pennsylvania State University, 104 Chemistry Building, University Park, PA 16802
Enantiomerically pure β-amino acids and their derivatives are important building blocks for the synthesis of β-peptides, β-lactam antibiotics and many important drugs. Recently, an efficient approach for the synthesis of protected β-amino acid derivatives has been developed in our group. Enamine substrates can be easily obtained through a one-step synthesis from the corresponding β-keto esters. The catalytic asymmetric hydrogenation afforded the desired products in high enantioselectivities