Trifluoroacetic acid → N-tert-butyl-2-fluoro-3-(piperazin-1-ylmethyl)benzamide

Participants

Reaction Steps

To a stirred mixture of tert-butyl 4-(3-(tert-butylcarbamoyl)-2-fluorobenzyl)piperazine-1-carboxylate (2.54 mmol, 1 g) in dichloromethane at room temperature was added trifluoro-acetic acid (53.9 mmol, 4 mL, 6.14 g). After 3 hours stirring the reaction was concentrated under reduced pressure. The residue was taken up in dichloromethane/methanol and loaded on to strong cation exchange column (10 g) and washed with dichloromethane/methanol. Elution of the column with 2M ammonia in methanol gave the title compound (636 mg). MS (ESI) m/z 294.4 [M+H]+

Provenance & Evidence