Hydrogen Bromide → 5-(trans-2-(2,6-Difluorobenzyl)piperidin-4-yl)isoxazol-3(2h)-one

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Reaction Steps

Trans-methyl 2-(2,6-difluorobenzyl)-4-(3-oxo-2,3-dihydroisoxazol-5-yl)piperidine-1-carboxylate (0.329 g, 0.93 mmol) was dissolved in hydrogen bromide (33% in acetic acid, 7.5 mL, 42.82 mmol) and the mixture was stirred at room temperature overnight. The solvent was evaporated and the residue purified by preparative HPLC (Instrument: FractionLynx II, Mobilphase: gradient 5-95% MeCN in 0.2% NH3, pH 10, Column: Xbridge Prep C18 5 μm OBD 19*150 mm) to yield 5-(trans-2-(2,6-difluorobenzyl)piperidin-4-yl)isoxazol-3(2H)-one (4.6 mg, 1.7%). HRMS Calculated for [C15H16F2N2O2+H]+: 295.1258. Found: 295.1257

Provenance & Evidence