Phosphorus oxychloride → 1-Chloro-7-(trifluoromethyl)phthalazine

Participants

Reaction Conditions

Reaction Steps

Into a 50 mL round-bottom flask, was placed 7-(trifluoromethyl)phthalazin-1-ol (prepared as described in the previous step, 1.6 g, 7.48 mmol, 1.00 equiv) and POCl3 (12 mL). The reaction mixture was stirred for 2 h at 100° C. in an oil bath. The resulting mixture was concentrated under vacuum. The residue was dissolved in 50 mL of dichloromethane, washed with 3×5 mL of H2O, dried (Na2SO4), and concentrated under vacuum. The residue was purified by chromatography over a silica gel column with CH3CN/H2O (10:4). The title compound was obtained as a yellow solid.

Provenance & Evidence