Trifluoroacetic acid → 1-(Oxetan-3-YL)piperidin-4-amine

Participants

Reaction Steps

To a solution of (1-oxetan-3-yl-piperidin-4-yl)-carbamic acid tert-butyl ester (134 mg, 0.52 mmol) in dichloromethane (2 mL) was added TFA (2 mL). After 15 minutes at ambient temperature the reaction mixture was concentrated in-vacuo and the residue loaded onto a 5 g SCX-2 cartridge which was washed with methanol, then 2N ammonia in methanol. Concentration of the combined basic fractions in-vacuo afforded the title compound as a colourless gum (82 mg, 100%). 1H NMR (400 MHz, CDCl3): 4.63-4.63 (m, 4H), 3.47-3.45 (m, 1H), 2.69-2.68 (m, 3H), 1.90-1.81 (m, 4H), 1.41-1.40 (m, 2H).

Provenance & Evidence