反应详情

To a solution of 2-ethyl-N-(3-fluoro-4-piperazin-1-yl-phenyl)-butyramide (0.08 g, 0.27 mmol) and Na2CO3 (0.03 g, 0.30 mmol) in DMF (2 mL) was added 2-bromo-2-phenyl-1-pyrrolidin-1-yl-ethanone (0.09 g, 0.30 mmol). After 18 h of stirring the mixture was diluted with EtOAc (30 mL) and washed with water (3×30 mL). The organic layer was dried (MgSO4) and concentrated. Chromatography of the resulting residue (SiO2; 2 M NH3 in MeOH/DCM) gave the title compound (0.08 mg, 51%). MS (ESI): mass calcd. for C28H37FN4O2, 480.29. m/z found, 481.4 [M+H]+. 1H NMR (DMSO): 7.52-7.47 (m, 3H), 7.36-7.29 (m, 3H), 7.07-7.05 (m, 1H), 6.87-6.83 (m, 1H), 3.42-3.38 (m, 1H), 3.09 (br s, 4H), 2.69 (s, 4H), 2.10-1.45 (m, 12H), 0.96-0.94 (m, 6H).

1. washwashed with water (3×30 mL)
2. dry with materialThe organic layer was dried (MgSO4)
3. concentrationconcentrated