反应详情

To a solution of tert-butyl(1-(4-(5-amino-6-(aminomethyl)-3-phenylpyridin-2-yl)phenyl)cyclobutyl)carbamate (113 mg, 0.25 mmol) in dry THF (2 ml) was added CDI (41 mg, 0.25 mmol) under nitrogen. The resulting mixture was stirred for 1 h at 60 C and concentrated to dryness under reduced pressure. The resulting residue was purified by Biotage silica gel chromatography (gradient 0 to 5% MeOH in DCM) to give the title compound (71 mg, 59%). 1H NMR (500 MHz, CDCl3): 8.91 (1H, br s), 7.19-7.11 (7H, m), 7.00-6.97 (3H, m), 5.73 (1H, s), 4.93 (1H, s), 4.65 (2H, s), 2.52-2.20 (4H, m), 2.00-1.95 (1H, m), 1.79-1.65 (1H, m), 1.40-1.10 (9H, br)

1. concentrationconcentrated to dryness under reduced pressure
2. customThe resulting residue was purified by Biotage silica gel chromatography (gradient 0 to 5% MeOH in DCM)