反应详情

温度

80 °C

To a solution of tert-butyl (3R)-3-((6-(5-(6-(1-methylethoxy)-2-pyrazinyl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazol-3-yl)-2-pyrazinyl)oxy)-1-piperidinecarboxylate (0.130 g, 0.21 mmol) in MeOH (2.0 mL) was added HCl (5 M in IPA, 4.2 mL, 21.11 mmol, Acros). The mixture was heated at 80° C. for 30 min. The crude reaction was cooled to RT and concentrated to a yellow solid that was slurried with a 1/1 mixture of DCM/MeOH (2 mL) and applied to a pre-washed (5 mL MeOH) of Si-propylsulfonic acid (Silicycle, Cat# R51230B). The column was washed with MeOH (10 mL). The compound was released with 15 mL of 2 M NH3 in MeOH to afford 5-(6-(1-methylethoxy)-2-pyrazinyl)-3-(6-((3R)-3-piperidinyloxy)-2-pyrazinyl)-1H-indazole as a pink solid. MS (ESI, pos. ion) m/z: 432.2 (M+1).

1. customThe crude reaction
2. temperaturewas cooled to RT
3. concentrationconcentrated to a yellow solid
4. additionthat was slurried with a 1/1 mixture of DCM/MeOH (2 mL)
5. washa pre-washed (5 mL MeOH) of Si-propylsulfonic acid (Silicycle, Cat# R51230B)
6. washThe column was washed with MeOH (10 mL)