反应详情

A mixture of 1-benzyl-5-cyano-8-hydroxy-2-oxo-1,2-dihydro-[1,6]naphthyridine-7-carboxylic acid methyl ester (20 mg, 0.060 mmol) and N-(2-amino-ethyl)-acetamide (20 mg, 0.18 mmol) in EtOH (3 mL) was refluxed for 16 h. After cooling to r.t., AcOH (0.1 mL), water (15 mL) and EtOAc (20 mL) were added. The aqueous layer was extracted with additional EtOAc, and the organic layers were combined, dried over MgSO4, and concentrated. The crude product was purified by silica gel chromatography (0-5% MeOH/CH2Cl2) to give 8.7 mg of the title compound as a light yellow solid. MS: (−) m/z 404.32 (M−1).

1. temperaturewas refluxed for 16 h
2. extractionThe aqueous layer was extracted with additional EtOAc
3. dry with materialdried over MgSO4
4. concentrationconcentrated
5. customThe crude product was purified by silica gel chromatography (0-5% MeOH/CH2Cl2)