Trifluoroacetic acid → N-[4-(4-amino-3-fluoro-phenoxy)-2-pyridyl]cyclopropanecarboxamide

Participants

Reaction Steps

Dissolve tert-butyl N-[4-[[2-(cyclopropanecarbonylamino)-4-pyridyl]oxy]-2-fluoro-phenyl]carbamate (12.14 g, 31.28 mmol) in DCM (280 mL), add trifluoroacetic acid (35 mL). Stir the reaction at room temperature for 5 hrs. Remove the volatiles under reduced pressure. Add EtOAc (300 mL), washed with saturated NaHCO3 solution (300 mL×2), and brine (300 mL×2). Dry the organic layer with anhydrous Na2SO4. Concentrate to give the crude product. Purification by chromatography (silica gel, EtOAc:PE=1:1) affords the title compound (7 g, 78.4%). MS: (M+1): 288.

Provenance & Evidence