反应详情

[(S)-1-(7-Bromo-6-methoxy-1-phenyl-1H-benzoimidazol-2-yl)ethyl]-[9-(tetrahydro-pyran-2-yl)-9H-purin-6-yl]amine (453 mg, 0.83 mmol) was dissolved in HCl in methanol (5 mL, 2.5M) and the reaction stirred at RT for 2 h. The reaction mixture was concentrated in vacuo and the resultant residue was subjected to preparative HPLC (C18 Phenomenex column, 10-90% MeCN in water 0.1% formic acid, 20 min gradient) to yield 272 as a white solid (70 mg, 18%). 1H NMR 400 MHz 6 (DMSO-d6): 8.08 (1H, br s), 8.02 (1H, s), 7.84 (1H, br s), 7.59 (1H, d, J=8.6 Hz), 7.55-7.26 (5H, m), 7.05 (1H, d, J=9.0 Hz), 5.15 (1H, br s), 3.79 (3H, s), 1.49 (3H, d, J=6.6 Hz). LCMS (Method K): RT=3.53 min, [M+H]+=464+466

1. concentrationThe reaction mixture was concentrated in vacuo
2. customC18 Phenomenex column, 10-90% MeCN in water 0.1% formic acid, 20 min gradient