铱催化体系不对称合成手性药物中间体(S)-(-)-1,1-二苯基-2-丙醇

Asymmetric Synthesis of Chiral Drug Intermediate( S)-( + )-1,1-Diphenyl-2-propanol by Iridium Catalytic System

考察了1,1-二苯基丙酮在手性双胺双膦配体与[IrHCl2(COD)]2组成的催化体系下不对称转移氢化合成(S)-(-)-1,1-二苯基-2-丙醇的反应,通过正交实验考察了反应温度、n(底物)∶n(铱络合物)、n(铱络合物)∶n(手性配体)以及n(底物)∶n(KOH)对反应的影响。结果表明,在异丙醇中,利用该体系催化1,1-二苯基丙酮反应2h后,产率可达97.85%,对映选择性(ee值)达到99.35%。

The iridium catalytic system diaminodiphosphine ligand was applied composed of the [ IrHC12 （COD）]2 and the chiral in the asymmetric transfer hydrogenation of 1, 1- diphenylacetone for the synthesis of （S）-（-）-1,1-diphenyl-2-propanol. The influence of temperature, substrate/catalyst molar ratio, metal complex/chiral ligand molar ratio and lye concentration on the reaction was investigated. The results show that 97.85 % of yield and 99. 35 % ee were achieved when 1,1-diphenylacetone was reduced for 2 h in this catalytic system.