铱催化体系不对称合成手性药物中间体

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

摘要:

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，通过正交实验了考察了反应温度、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2小时后，反应产率可达97.85%，对映选择性(ee值)达到99.35%

Abstract:

The iridium catalytic system composed of the [ IrHCl2( COD )]2 and the chiral diaminodiphosphine ligand was applied in the asymmetric transfer hydrogenation of 1,1-diphenylacetone in 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 tested. The results show that 97.85% of yield and 99.35% ee were achieved when 1,1-dphenylacetone was reduced for 2 h in this catalytic system.