Phosphorus oxychloride → 6-Bromo-2-chloro-8-methoxyquinazoline

Participants

Reaction Conditions

Reaction Steps

A suspension of 6-bromo-8-methoxyquinazolin-2-ol (43.96 mmol) in POCl3 (120 mL) was heated to 110° C. for 30 minutes The mixture was cooled to room temperature, evaporated POCl3 and partitioned between water and dichloromethane. The organic portion was concentrated to give a crude material which was purified by column chromatography (silica gel, eluted with 2% MeOH in dichloromethane) to yield pure material as a yellow solid in 30% yield (3 steps, 3.62 g). ES/MS m/z 272/274 (MH+).

Provenance & Evidence