反应详情

温度

80 °C

To a suspension of N-(cis-4-aminocyclohexyl)isobutyramide hydrochloride (200 mg, 0.906 mmol) and DIPEA (0.432 mL, 2.471 mmol) in ACN (2 mL) was added (3-fluoro-4-nitrophenyl)methanol (141 mg, 0.824 mmol). The reaction was stirred overnight at 80° C. After 16 hours, the reaction mixture was concentrated and the residue purified by column chromatography, eluting with 0-100% EtOAc in DCM, to provide N-(cis-4-(5-(hydroxymethyl)-2-nitrophenylamino)cyclohexyl)isobutyramide as an orange foam (176 mg, 63.7% yield). MS, m/z (C17H25N3O4): calcd, 335.2. found, 336.0 [M+H].

1. waitAfter 16 hours
2. concentrationthe reaction mixture was concentrated
3. customthe residue purified by column chromatography
4. washeluting with 0-100% EtOAc in DCM