Acetic Acid → HCID 86685926, compound

Participants

Reaction Steps

N-[2-(3-Chloro-4-fluoro-phenyl)-ethyl]-2,2,2-trifluoro-acetamide (400 mg, 1.48 mmol) and paraformaldehyde (89 mg, 2.96 mmol) were added sequentially at 0° C. to a solution of acetic acid (3 mL) in sulfuric acid (2 mL). After stirring of the reaction mixture at room temperature for 16 hours, the clear colorless solution was poured into ice-water (20 mL). The mixture was extracted with EtOAc (2×30 mL) and the organic layer was washed with satd. aq. NaHCO3 (20 mL), H2O (2×25 mL), dried over anhy. Na2SO4, filtered and concentrated in vacuo to give the crude title product together with a regioisomer (400 mg) as white solid.

Provenance & Evidence