反应详情

A solution of (S)-4-(benzyloxy)-1-(1-(2-(3-fluoropyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one (56 mg, 0.12 mmol) in CH2Cl2 (1.5 mL) was treated with anhydrous HCl in diethyl ether (0.12 mL, 0.12 mmol, 1.0 M). The reaction mixture was stirred at ambient temperature for 2 h, and then the solids were collected by filtration and dried to yield the title compound (51.4 mg, 85%) as a white powder: mp 197-200° C.; 1H NMR (500 MHz, DMSO-d6) δ 10.62-10.50 (m, 1H), 8.25 (s, 1H), 7.85 (d, J=8.0 Hz, 1H), 7.80 (s, 1H), 7.61 (d, J=7.5 Hz, 1H), 7.48-7.42 (m, 5H), 7.39-7.36 (m, 1H), 6.13 (dd, J=7.5, 3.0 Hz, 1H), 5.99 (d, J=2.5 Hz, 1H), 5.54-5.39 (m, 1H), 5.16 (s, 2H), 4.87-4.82 (m, 2H), 3.81-3.53 (m, 4H), 3.55-3.20 (m, 2H, overlapping with H2O peak), 2.14-2.01 (s, 2H); ESI MS m/z 433 [M+H]+; HPLC (Method A)>99% (AUC), tR=14.4 min; optical rotation [α]22.5D-8.4° (c 0.095, Methanol).

1. filtrationthe solids were collected by filtration
2. customdried