Trifluoroacetic acid → 1-(2-Methoxyethyl)piperidin-4-amine

関与物質

反応手順

A mixture of tert-butyl 1-(2-methoxyethyl)piperidin-4-ylcarbamate (0.842 g, 3.26 mmol) and 2,2,2-trifluoroacetic acid (2.51 ml, 32.6 mmol) was stirred for 15 minutes at ambient temperature. The mixture was concentrated in vacuo, using toluene (2×10 mL) to azeotrope residual TFA. The crude TFA salt of the product was converted to the free base using Biotage Flash 40M flash chromatography, eluting with 10% MeOH (containing 7N NH3) in DCM (500 mL), followed by 20% MeOH (containing 7N NH3) in DCM (500 mL). The product was obtained as an oil (195 mg, 37%).

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