反应详情

To a solution of (R)-tert-butyl 6-hydroxy-6-methyl-4-(6-(6-(1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)-1H-pyrazolo[4,3-c]pyridin-1-yl)pyridin-2-yl)-1,4-diazepane-1-carboxylate (46 mg, 0.08 mmol) in MeOH (3 mL) was added HCl solution (conc. 3.0 mL) and stirred at room temperature for 4 hours. The mixture was concentrated under reduced pressure. The crude was purified by reverse phase preparative HPLC to afford 248 as a white solid (36 mg, 94%). 1H NMR (500 MHz, DMSO-d6) δ (ppm) 9.16 (s, 1H), 8.77 (s, 1H), 8.54 (s, 1H), 8.50 (s, 1H), 8.25 (s, 1H), 7.67 (t, 1H), 7.12 (d, 1H), 6.72 (d, 1H), 5.25-5.20 (t, 2H), 4.68 (s, 1H), 4.03-4.00 (m, 2H), 3.57-3.48 (m, 2H), 3.08-3.06 (m, 2H), 2.72 (d, 1H), 2.60 (d, 1H), 1.14 (s, 3H); MS (ESI) m/z: 473 [M+H]+.

1. concentrationThe mixture was concentrated under reduced pressure
2. customThe crude was purified by reverse phase preparative HPLC