Hydrochloric Acid → HCID 10628651, compound

Participants

Reaction Steps

To a solution of the objective compound (450 mg, 0.651 mmol) of Step (1), ethylamine hydrochloride (67 mg, 0.82 mmol) and HOBT (176 mg, 1.30 mmol) in DMF (10 mL) were added N-ethylmorpholine (0.10 mL, 0.79 mmol) and WSCI hydrochloride (148 mg, 0.772 mmol) and the mixture was stirred at room temperature for 3.5 hours. The reaction mixture was added to 1N hydrochloric acid (80 mL) and extracted with ethyl acetate. The extract was washed successively with a saturated aqueous sodium hydrogencarbonate solution and saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The obtained solid was washed with ether and dried in vacuo to give 2-[5-benzyloxycarbonylamino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[[5-(ethylaminocarbonyl)benzoxazol-2-yl]hydroxymethyl]-2-phenylethyl]acetamide as a white solid (397 g, 85%).

Provenance & Evidence