反应详情

4-{4-[6-Amino-5-(5-chloro-6,8-difluoroisoquinolin-3-yl)-pyridin-3-yl]-pyrazol-1-yl}-piperidine-1-carboxylic acid tert-butyl ester (0.0311 mmol) was dissolved in DCM (4.4 ml), and 1.0 M of HCl in Et2O (8.8 ml) was added. The mixture was stirred at rt for 16 h. After that time, solvent was removed in vacuo to give the title compound as a yellow powder. 1H NMR (400 MHz, DMSO-d6): δ=2.14-2.30 (m, 4H), 3.03-3.18 (m, 2H), 3.36-3.42 (m, 2H), 4.50-4.60 (m, 1H), 4.97 (brs, 2H), 8.07 (t, J=10.0 Hz, 1H), 8.14 (s, 1H), 8.49 (s, 1H), 8.53 (d, J=2.4 Hz, 1H), 8.63 (d, J=0.8 Hz, 1H), 8.81 (d, J=2.4 Hz, 1H), 9.14 (brs, 1H), 9.31 (brs, 1H), 9.66 (s, 1H). MS(ES+): m/z=440.84/442.79 (82/32) [MH+]. HPLC: tR=1.89 min (ZQ3, polar—5 min).

1. customAfter that time, solvent was removed in vacuo