钯催化α-(6-甲氧基-2-萘基)乙醇的不对称羰基化反应

Asymmetric Carbonylation of α (6 Methoxy 2 naphthyl)ethanol by PdCl 2 CuCl 2 p Ts Chiral Phosphine Catalyst Systems

不对称羰基化可产生多种手性分子，而这些手性分子是合成药物和农药等重要前体［１］．光学活性的α－芳基丙酸类如Ｓ－布洛芬和萘普生是很重要的非麻醉性镇痛消炎药．以不对称氢甲酰化反应和氢羧基化反应制备光学活性的布洛芬和萘普生已有报道［２，３］，但这些不对称羰...

α (6 Methoxy 2 naphthyl)ethanol was carbonylated to methyl ester of Naproxen by PdCl 2 CuCl 2 p Ts chiral phosphine catalyst systems under the mild reaction conditions. Poor enantioselectivities and moderate regioselectivities have been obtained by using the ligand DDPPI for PdCl 2 CuCl 2 p Ts catalytic reaction. The effects of P/Pd molar ratio, reaction pressure, and the kinds of solvents have been also investigated with the catalyst system. The asymmetric induction up to 42.5 and good chemical yields have been obtained in the carbonylation of α (6 methoxy 2 naphthyl)ethanol with carbon monooxide and alcohol.