Phosphorus oxychloride → 4-Chloro-7-ethoxy-6-methoxyquinazoline

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Reaction Steps

A mixture of 7-ethoxy-6-methoxyquinazolin-4(3H)-one (1.20 g, 5.45 mmol) and POCl3 (3 mL), in toluene (10 mL) was heated at 125° C. for 5 hours. It was concentrated under reduced pressure to dryness. To it was added CH2Cl2 and it was washed with saturated NaHCO3. The organic layer was dried over MgSO4 and concentrated to give 4-chloro-7-ethoxy-6-methoxyquinazoline as solid (1.254 g, 96%). 1H NMR (300 MHz, CDCl3) δ 8.91 (s, 1H), 7.52 (s, 1H), 7.42 (s, 1H), 4.34 (q, 2H), 4.08 (s, 3H), 1.59 (t, 3H).

Provenance & Evidence