反应详情

温度

43 °C

To a solution of 7-fluoro-2-(methyloxy)-8-[(2S)-2-oxiranyl]-1,5-naphthyridine (220 mg, 1.0 mmol) in acetonitrile (5 mL) were added phenylmethyl[(3R)-3-pyrrolidinylmethyl]carbamate (235 mg, 1.0 mmol) followed by Lithium perchlorate (106 mg, 1.0 mmol). After heated at 43° C. for 48 h, the resulting mixture was cooled down to room temperature, concentrated and purified with column chromatography (silica, 1-5% methanol in DCM (1% NH4OH)) to provide the title compound as an off-white solid (250 mg, 55%): LC/MS (ES) m/e 455 (M+H)+.

1. temperaturethe resulting mixture was cooled down to room temperature
2. concentrationconcentrated
3. custompurified with column chromatography (silica, 1-5% methanol in DCM (1% NH4OH))