反应详情

A solution of (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-ethylazepan-2-one (135 mg, 0.503 mmol) in dichloromethane was treated N,N-diisopropylethylamine (65 mg, 0.503 mmol) and diphenyl N-cyanocarbonimidate (204 mg, 0.855 mmol). After 5 h, the reaction was quenched with 0.5N NaOH and the organic layer washed with water and brine. The combined aqueous layers were extracted with EtOAc. The combined organics were dried, filtered and concentrated. Purification by silica gel chromatography (EtOAc/hexanes) gave the title compound (166 mg). MS 413.3 (M+1).

1. customthe reaction was quenched with 0.5N NaOH
2. washthe organic layer washed with water and brine
3. extractionThe combined aqueous layers were extracted with EtOAc
4. customThe combined organics were dried
5. filtrationfiltered
6. concentrationconcentrated
7. customPurification by silica gel chromatography (EtOAc/hexanes)