铑(I)催化的不对称硅氢化反应合成手性2-氨基-1-芳基乙醇研究

Synthesis of α-Amino Alcohols via Rh(I)-catalytic Asymmetric Hydrosilylation of Amino Ketones

报道了以 Rh( ) -手性 2 -( 2 -吡啶基 ) -4 -羧甲基 -1 ,3-噻唑烷为催化剂 ,2 -氨基芳香酮的不对称硅氢化反应 ,在常温常压下手性 2 -氨基 -1 -芳基乙醇的产率几乎可达定量 ,产品光学纯度可达 80 % e.

The asymmetric hydrosilylation of 2 amino aryl ketones catalyzed by 2/2 (2 pyridyl) 4 carbomethoxy 1,3 thiazolidine(A) systems was first reported. The chiral 2 amino 1 aryl ethanols were obtained in nearly quantatative yield and high enantioselectivity. The reaction of fourteen 2 amino arylketones with different groups were investigated. It was found that the \%e.e.\% values were all higher than 92% when there are group(s), such as OH, OMe or Me on the phenyl group,while the optical purities were less than 85% e.e. when there are group(s) such as Cl, NO 2 on the phenyl group. In comparision with the reaction of ketones having no founctional group, the optical yield of 2 amino ketones were higher.