反应详情

To a solution of 3-amino-5-(2-oxo-pyrrolidin-1-yl)-benzoic acid (D6) (2.2 g, 10 mmol, 1 equiv) in MeOH/Et2O (1:1, 20 ml) was added 1-(3-dimethylaminopropyl)-3-ethyl-carbodiimide hydrochloride (2.3 g, 12 mmol, 1.2 equiv), DMAP (112 mg, 1 mmol, 0.1 equiv) and the resulting mixture was stirred at room temperature for 16 h then diluted with AcOEt. The organic phase was washed with saturated aqueous NaHCO3 solution, dried over MgSO4 and concentrated in vacuo. The residue was triturated with Et2O to give 3-amino-5-(2-oxo pyrrolidin-1-yl)-benzoic acid methyl ester (D4a) (1.6 g, 68%) as a white solid.

1. washThe organic phase was washed with saturated aqueous NaHCO3 solution
2. dry with materialdried over MgSO4
3. concentrationconcentrated in vacuo
4. customThe residue was triturated with Et2O