Hydrochloric Acid → 3-(2-Fluoro-4-(methylsulfonyl)phenylamino)-1,4'-bipiperidin-2-one

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Reaction Steps

Tert-butyl 3-(2-fluoro-4-(methylsulfonyl)phenylamino)-2-oxo-1,4′-bipiperidine-1′-carboxylate (7.9 g, 17 mmol) was dissolved in CH2Cl2 (100 mL) and MeOH (10 mL). 4N HCl in dioxane (29 mL, 118 mmol) was added and the reaction stirred at ambient temperature for 3 hours. The reaction was concentrated and purified over silica gel (50-100% EtOAc in hexanes followed by 5% ammoniated methanol in CH2Cl2) to afford 3-(2-fluoro-4-(methylsulfonyl)phenylamino)-1,4′-bipiperidin-2-one (6.2 g, 17 mmol, 100% yield) as yellow solid.

Provenance & Evidence