Trifluoroacetic acid → Cyclobutanamine,1-(2-pyridinyl)-

Participants

Reaction Steps

Crude (1-pyridin-2-yl-cyclobutyl)-carbamic acid tert-butyl ester (7.0 g, 5.64 mmol) was dissolved in DCM (20 mL) and TFA (20 mL) was added dropwise. After 6 h, the reaction was concentrated in vacuo and partitioned between DCM (100 mL) and water (20 mL). The aqueous layer was extracted with DCM (2×50 mL). The aqueous layer was then concentrated in vacuo. The brown oil was dissolved in water (3 mL) and purified via Mass-directed reverse phase HPLC purification which yielded 322 mg of 1-pyridin-2-yl-cyclobutylamine as a formic acid salt (yellow solid), m/z=149.5 [M+1]+.

Provenance & Evidence