Reaktion #718366

Reaktionsgleichung

formamide

acetic acid

2-amino-4,5-difluorobenzoic acid

→

6,7-difluoro-4-hydroxyquinazoline

Ausbeute 84.0%

Lösungsmittel

H2O

Reaktionsbedingungen

Aufarbeitung

1. 1
   TemperaturAfter cooling to room temperature
2. 2
   Filtrationthe resulting solid filtered
3. 3
   Sonstigedried under vacuum

Vorschrift

To a stirring mixture of formamide (10 mL) and glacial acetic acid (2.5 mL) was added 2-amino-4,5-difluorobenzoic acid (2.0 g, 11.6 mmol) and the solution stirred at 125° C. for 8 hours. After cooling to room temperature, the reaction was diluted with H2O (100 mL) and the resulting solid filtered and dried under vacuum to give 6,7-difluoro-4-hydroxyquinazoline (1.77 g, 9.7 mmol, 84%). 1H NMR (300 MHz, DMSO-d6) δ 12.49 (br s, 1H), 8.15 (s, 1H), 8.04 (dd, 1H), 7.76 (dd, 1H); LC-MS (ESI) m/z 183 (M+H)+.

Quelle