4-取代-2,4-二羰基丁酸酯的不对称转移氢化反应研究及应用

Asymmetric transfer hydrogenation of γ-aryl α,γ-dioxobutyric acid esters and its application

在(R,R)-RuCl(Fsdpen)(p-cymene)催化下进行了4-芳基-2,4-二羰基丁酸酯的不对称氢转移反应研究。考察了溶剂和温度对反应的影响;并以DMF为溶剂在0℃时进行了7种4-芳基-2,4-二羰基丁酸酯的不对称转移氢化(ATH)反应,得到高达85%产率和96%ee的反应产物;同时探索了(2R,4S)-α-羟基-γ-苯基-丁内酯的不对称合成。

The probe of the asymmetric transfer hydrogenation（ ATH） of a series of γ-aryl-α,γ-dioxo-butyric acid esters had been conducted with（ R,R）-Ru Cl（ Fsdpen）（ p-cymene） as catalyst.The reaction conditions were optimized and seven substrates＇ ATH proceeded smoothly.Up to 85%chemical yields and 96%ee were obtained.Simultaneously,the synthesis of a trans-2,4-disubstituted butyrolactone could also be achieved with a yield of 45%.