反应详情

HOBT (168 mg, 1.24 mmol), 5-chloroindole-2-carboxylic acid (243 mg, 1.24 mmol), DIPEA (0.22 mL, 1.24 mmol) and then EDCI (296 mg, 1.55 mmol) were added to a solution of (3-amino-2-oxo-3,4-dihydroquinolin-1(2H)-yl)acetonitrile (Method 12, 250 mg, 1.24 mmol) in DCM (10 mL). The reaction was stirred for 18 h at ambient temperature, diluted with EtOAc (15 mL), washed with 1 N NaOH (15 mL), 1 N HCl (15 mL), saturated aqueous NaHCO3 solution (15 mL), dried (MgSO4) and the volatiles removed under reduced pressure to give the title compound (366 mg, 78%) as a tan solid.

1. washwashed with 1 N NaOH (15 mL), 1 N HCl (15 mL), saturated aqueous NaHCO3 solution (15 mL)
2. dry with materialdried (MgSO4)
3. customthe volatiles removed under reduced pressure