反应详情

To a vigorously stirred solution of sodium hydrogen cyanamide (0.64 g, 10.0 mmol) in methanol (10 mL) was added dropwise 2-(4-fluoro-phenoxymethyl)-oxirane (1.68 g, 10 mmol) after which the reaction mixture was stirred at room temperature overnight. The reaction mixture was concentrated to remove methanol. Anhydrous diethyl ether (50 mL) was added after which the resulting white precipitate was removed by filtration through celite and the filtrate concentrated. The residue was purified by flash chromatography (silica, 7N NH3 in methanol/methylene chloride) to give 0.77 g (37%) of 5-(4-fluorophenoxymethyl)-(4,5-dihydro-oxazol-2-yl)amine.

1. concentrationThe reaction mixture was concentrated
2. customto remove methanol
3. additionAnhydrous diethyl ether (50 mL) was added after which the resulting white precipitate
4. customwas removed by filtration through celite
5. concentrationthe filtrate concentrated
6. customThe residue was purified by flash chromatography (silica, 7N NH3 in methanol/methylene chloride)