Preparation of 6-aminoquinazolin-4(3H)-ones via direct SNAr on the quinazoline ring

The preparation of 6-aminoquinazolin-4(3H)-ones requires the use of platinum–metal group catalysis on the corresponding C-6-iodo or 6-bromo precursors. Herein, we report to our knowledge the first successful SNAr reaction directly at the unactivated C-6 position of the quinazolin-4(3H)-one nucleus.