2-Amino-5-methoxybenzene-1,3-diol → 2-(2,5-Difluorophenyl)-6-methoxy-1,3-benzoxazol-4-ol

Participants

Reaction Conditions

Reaction Steps

2.8 g (9.02 mmol; 1 equivalent) of methyl 2,5-difluorobenzene carbimidothioate hydroiodide in solution in 20 ml of ethanol is added to a solution of 1.4 g (9.02 mmol) of 2-amino-5-methoxybenzene-1,3-diol in 80 ml of ethanol. The reaction mixture is maintained under stirring at 78° C. for 5 hours then the solvent is evaporated off under reduced pressure. The residue is purified by chromatography on a silica column (eluent: dichloromethane/methanol mixture 98:2) and 860 mg (34% yield) of 2-(2,5-difluorophenyl)-6-methoxy-1,3-benzoxazol-4-ol is obtained.

Provenance & Evidence