反应详情

To a mixture of N-Boc-L-proline (1.0 g, 4.65 mmol), aniline (0.433 g. 4.65 mmol), and HOBT (0.753 g, 5.58 mmol) in 10 mL of CH2Cl2 was added EDC (1.07 g, 5.58 mmol) and the solution was stirred overnight. To the solution was added 70 mL of EtOAc and washed with 50 mL 3N HCl, 50 mL water, 50 mL NaHCO3 (sat.), 50 mL 10% K2CO3, and 50 mL brine. The organic layer was then dried over MgSO4, filtered and concentrated under reduced pressure to give a white solid (1.2 g. 89%. ES (+) MS m/e=291 (M+H).

1. washwashed with 50 mL 3N HCl, 50 mL water, 50 mL NaHCO3 (sat.), 50 mL 10% K2CO3, and 50 mL brine
2. dry with materialThe organic layer was then dried over MgSO4
3. filtrationfiltered
4. concentrationconcentrated under reduced pressure
5. customto give a white solid (1.2 g. 89%. ES (+)