1042939-73-0Relevant articles and documents
Enantioselective Syntheses of (-)-(R)-Rolipram, (-)-(R)-Baclofen and Other GABA Analogues via Rhodium-Catalyzed Conjugate Addition of Arylboronic Acids
Becht, Jean-Michel,Meyer, Oliver,Helmchen, Guenter
, p. 2805 - 2810 (2003)
Highly enantioselective syntheses of two important γ-aminobutyric acid (GABA) analogues, the antispastic drug (-)-(R)-Baclofen and the antidepressant agent (-)-(R)-Rolipram, are reported. Key-steps in both syntheses are the Rh-catalyzed asymmetric 1,4-additions of arylboronic acids to 4-aminobut-2,3-enoic acid derivatives.
Enantioselective synthesis of (-)-(R)-Baclofen and analogues via rhodium-catalysed conjugate addition of boronic acids
Meyer, Oliver,Becht, Jean-Michel,Helmchen, Günter
, p. 1539 - 1541 (2003)
Highly enantioselective syntheses of the antispastic drug (-)-(R)-Baclofen and analogues have been achieved by using rhodium-catalysed asymmetric 1,4-additions of arylboronic acids to 4-amino-but-2,3-enoic acid derivatives.
Rh-catalyzed asymmetric hydrogenation of γ-phthalimido-substituted α,β-unsaturated carboxylic acid esters: An efficient enantioselective synthesis of β-aryl-γ-amino acids
Deng, Jun,Duan, Zheng-Chao,Huang, Jia-Di,Hu, Xiang-Ping,Wang, Dao-Yong,Yu, Sai-Bo,Xu, Xue-Feng,Zheng, Zhuo
, p. 4825 - 4828 (2008/03/15)
(Chemical Equation Presented) A series of chiral β-aryl-γ-amino acid ester derivatives were synthesized in high enantioselectivities (93-97% ee) via the Rh-catalyzed asymmetric hydrogenation of γ-phthalimido-α, β-unsaturated carboxylic acid esters using highly modular chiral BoPhoz-type phosphine-aminophosphine ligands. The method has been applied successfully to the synthesis of several chiral pharmaceuticals including (R)-baclofen and (R)-rolipram with high enantioselectivities.