Rhodium-catalyzed asymmetric addition of arylboronic acids to γ-phthalimido-substituted-α, β-unsaturated carboxylic acid esters: an approach to γ-amino acids
F Han, J Chen, X Zhang, J Liu, L Cun, J Zhu, J Deng…
Efficient Rh-catalyzed asymmetric 1, 4-addition of arylboronic acids to ethyl-γ- phthalimidocrotonate by using bis-sulfoxide ligand affords γ-aminobutyric acid (GABA) derivatives with high enantioselectivities (90–96% ee) under mild conditions. Optically pure (S)-Baclofen and (S)-Rolipram have been prepared successfully through this synthetic route.
