Triethylamine hydrochloride → 2,4-Dichloro-6-piperidinoquinazoline

Participants

Reaction Steps

To 6-Piperidin-1-yl-1H-quinazoline-2,4-dione (522 mg, 2.13 mmol) and triethyl amine hydrochloride (1.2 g, 8.5 mmol) was added POCl3 (20 mL) and the solution was heated to 120 C for 72 h. POCl3 was removed in vacuum and the resulting brown oil was quenched with ice water and treated with saturated NaHCO3, to afford a tan solid. Filtration and drying in vacuum gave title compound 550 mg (91% yield). HPLC tr=8.56 min (100%), FIA m/z 282.1 (M+H), HNMR (500 MHz, dmso): 8.05-8.00 (1H, d), 7.85-7.80 (1H, d), 7.20 (1H, s), 5.50-4.40 (4H, m), 1.70-1.60 (6H, m).

Provenance & Evidence