反应详情

To a solution of tert-butyl(1-(4-(2-oxo-7-phenyl-2,3-dihydro-1H-pyrido[2,3-b][1,4]oxazin-6-yl)phenyl)cyclobutyl)carbamate (19 mg, 0.04 mmol) in dry DMF (1 mL) was added potassium carbonate (12 mg, 0.08 mmol) and 2-chloroacetamide (12 mg, 0.12 mmol) at room temperature under nitrogen. The reaction mixture was stirred overnight at room temperature and concentrated to dryness under reduced pressure. The resulting residue was purified by silica gel chromatography (gradient 0 to 80% AcOEt in hexane) to give the title compound (14 mg, 67%). 1H NMR (500 MHz, CDCl3): 7.32 (1H, s), 7.28-7.23 (7H,m), 7.16-7.14 (2H,m), 6.22 (1H, br s), 5.65 (1H, br s), 5.09 (1H, br s), 4.94 (2H, s), 4.52 (2H,s), 2.55-2.25 (4H, m), 2.09-2.01 (1H, m), 1.85-1.76 (1H, m), 1.44-1.15 (9H, br).

1. concentrationconcentrated to dryness under reduced pressure
2. customThe resulting residue was purified by silica gel chromatography (gradient 0 to 80% AcOEt in hexane)