反应详情

To a solution of tert-butyl 4-(6-(6-(1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)-1H-pyrazolo[4,3-c]pyridin-1-yl)pyrazin-2-yl)-1,4-diazepane-1-carboxylate (80 mg, 0.147 mmol) in 1,4-dioxane (6 mL) was added a solution of HCl/1,4-dioxane (3.8 M, 6 mL). The reaction mixture was stirred at room temperature for 2 hours and concentrated under reduced pressure to give a crude product. The crude was purified by reverse phase preparative HPLC to afford 178 as a white solid (55 mg, 84%). 1H NMR (500 MHz, DMSO-d6) δ (ppm) 9.17 (s, 1H), 8.60 (s, 1H), 8.54 (s, 1H), 8.37 (d, J=6.0 Hz, 2H), 8.09 (s, 1H), 8.02 (s, 1H), 5.26 (Q, J=9.2 Hz, 2H), 3.86 (s, 2H), 3.81 (s, 2H), 3.01 (t, J=5.5 Hz, 2H), 2.76 (t, J=5.5 Hz, 2H), 1.89 (t, J=5.5 Hz, 2H). MS (ESI) m/z: 444 [M+H]+.

1. concentrationconcentrated under reduced pressure
2. customto give a crude product
3. customThe crude was purified by reverse phase preparative HPLC