Hydrochloric Acid → (S)-3-(1H-indazol-5-yloxy)-1-(piperidin-4-yl)pyrrolidin-2-one

Participants

Reaction Steps

A flask was charged with (S)-tert-butyl 4-(3-(1H-indazol-5-yloxy)-2-oxopyrrolidin-1-yl)piperidine-1-carboxylate (0.300 g, 0.749 mmol), HCl in dioxane (1.87 mL, 7.49 mmol), DCM (10 mL), and methanol (1 mL). The reaction was stirred at ambient temperature for 2 hours. The organic solvents were removed under reduced pressure. The residue was purified using silica gel column chromatography using 50-100% ethyl acetate in hexanes, then 5% ammoniated methanol in DCM, and then 30% ammoniated methanol in ethyl acetate to provide (S)-3-(1H-indazol-5-yloxy)-1-(piperidin-4-yl)pyrrolidin-2-one (0.225 g, 100% yield).

Provenance & Evidence