Ammonium Hydroxide → 4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxyquinazolin-6-ol

Participants

Reaction Steps

To a solution of 6-acetoxy-4-(3-chloro-4-fluoro-phenylamino)-7-methoxy-quinazoline (1.54 g, 4.26 mmol) (from Example 18, Step A, supra) in MeOH (30 mL) was added an aqueous solution of NH4OH (29%, 0.86 mL, 12.7 mmol). The reaction mixture was stirred at room temperature for 18 hours, then heated at 100° C. for 1.5 hours. The mixture was then cooled to room temperature and filtered. The precipitate was collected and dried in vacuo to give the desired 4-(3-chloro-4-fluoro-phenylamino)-7-methoxy-quinazolin-6-ol as a gray solid. (Yield 1.21 g, 89%).

Provenance & Evidence