反应详情

To a solution of 3-amino-1-benzhydryl-pyrrolidin-2-one (42) (0.2 g, 0.75 mmol) in dry CH2Cl2 (20 ml)was added diphenylamino ethanoic acid (0.19 g, 0.82 mmol) under nitrogen. To the reaction was added EDC (0.18 g, 0.9 mmol) and DMAP (cat) and the reaction mixture was stirred under nitrogen at room temperature overnight. The reaction was then concentrated under reduced pressure. The residue was dissolved in ethyl acetate:water (10:1) (100 ml). The organic was washed with water (25 ml, 2×) and 10% NaOH (25 ml), dried over MgSO4 and evaporated to dryness. The resulting residue was purified by column chromatography using hexane:ethyl acetate (2:1) to give the desired product in 69% yield.

1. concentrationThe reaction was then concentrated under reduced pressure
2. dissolutionThe residue was dissolved in ethyl acetate:water (10:1) (100 ml)
3. washThe organic was washed with water (25 ml, 2×) and 10% NaOH (25 ml)
4. dry with materialdried over MgSO4
5. customevaporated to dryness
6. customThe resulting residue was purified by column chromatography