WalPhos配体/铑配合物对β,γ-不饱和膦酸酯的不对称催化氢化

Rh-catalyzed Asymmetric Hydrogenation of β,γ-Unsaturated Phosphonates with WalPhos Ligands

用手性配体(R c,S p)-WalPhos与铑形成的配合物为催化剂,在1.0 MPa的氢气压力、二氯甲烷溶剂中以及室温的反应条件下,对β-取代β,γ-不饱和膦酸酯底物进行不对称催化氢化,合成了具有β-手性中心的手性膦酸酯类化合物,所有考察的底物均可完全转化,最高获得了87%的ee值。

An enantioselective synthesis of chiral alkylphosphonates bearing a β-stereogenie center, based on the Rh-catalyzed asymmetric hydrogenation of corresponding β-substitutedβ,γ-unsaturated phosphonates with （Re, Sp ）-WalPhos ligand under the mild hydrogenation temperature）, was developed. The full conversions can be conditions （1.0 MPa hydrogen pressure and room achieved and an ee value of up to 87 % is obtained.