反应详情

Intermediate 42 (212 mg, 0.495 mmol) was dissolved in EtOAc (2 ml), treated with 4M HCl in dioxane (1.61 ml, 6.44 mmol) and stirred overnight at room temperature. The mixture was concentrated in vacuo, treated with EtOAc and concentrated again. This process was repeated 5 times. The resulting white solid was triturated with Et2O, filtered, rinsed with Et2O and dried in a vacuum oven at 50° C. to afford 155 mg (86%) of the title product—1-(4-chloro-phenyl)-3-(piperidin-4-yloxy)-1H-indazole hydrochloride as a white solid.

1. concentrationThe mixture was concentrated in vacuo
2. additiontreated with EtOAc
3. concentrationconcentrated again
4. customThe resulting white solid was triturated with Et2O
5. filtrationfiltered
6. washrinsed with Et2O
7. customdried in a vacuum oven at 50° C.