反应详情

4-{4-[6-Amino-5-(5,8-difluoro-3,4-dihydro-1H-isoquinolin-2-yl)-pyridin-3-yl]-pyrazol-1-yl}-piperidine-1-carboxylic acid tert-butyl ester (26 mg, 0.051 mmol) was dissolved in MeOH (20 mL), 1.0 M of HCl in Et2O (20 mL) was added, and the mixture was stirred at rt overnight. The solvent was removed in vacuo to give the title compound as a brown solid. 1H NMR (400 MHz, CD3OD): δ=2.33-2.42 (m, 4H), 3.08 (t, J=5.2 Hz, 2H), 3.23-3.36 (m, 2H), 3.39 (t, J=5.6 Hz, 2H), 3.59 (d, J=12.8 Hz, 2H), 4.24 (s, 2H), 4.62-4.72 (m, 1H), 6.99-7.04 (m, 2H), 7.97 (s, 1H), 8.01 (s, 1H), 8.07 (s, 1H), 8.39 (s, 1H). MS(ES+): m/z=411.08 (42) [MH+]. HPLC: tR=2.10 min (ZQ2, polar—5 min).

1. customThe solvent was removed in vacuo