Phosphorus oxychloride → 6-Bromo-4-chloro-2-(methylsulfanyl)quinazoline

Participants

Reaction Steps

Diisopropylethylamine (0.65 ml, 3.69 mmol) was added to a suspension of 6-bromo-2-(methylthio)-quinazolin-4-ol (500 mg, 1.85 mmol) in POCl3 (6.5 ml). The reaction was heated at reflux for 6 hours and then cooled to room temperature. The POCl3 was removed under reduced pressure. The residue was diluted with EtOAc (30 ml) and poured onto ice. The organic layer was washed twice with brine (2×30 ml), then dried over sodium sulfate and concentrated. The product thus obtained was used without further purification.

Provenance & Evidence