反应详情

A mixture of 7-benzyl-4-hydroxy-8-oxo-7,8-dihydro-[2,7]naphthyridine-3-carboxylic acid methyl ester (50 mg, 0.16 mmol), 4-aminobutyric acid (832 mg, 8.06 mmol) and NaOMe solution (12 mL, 6.05 mmol, 0.5 M in MeOH) was refluxed for 48 h. Solvent was evaporated in vacuo, and the residue was partitioned between water and EtOAc. 1 M HCl was added with vigorous stirring until pH was about 2. The organic layer was dried over MgSO4 and concentrated. The crude product was purified by silica gel chromatography (5-60% EtOAc/hexanes+2% AcOH) to give 31 mg of the title compound as a light yellow solid. MS: (+) m/z 382.01 (M+1).

1. temperaturewas refluxed for 48 h
2. customSolvent was evaporated in vacuo
3. customthe residue was partitioned between water and EtOAc
4. addition1 M HCl was added
5. dry with materialThe organic layer was dried over MgSO4
6. concentrationconcentrated
7. customThe crude product was purified by silica gel chromatography (5-60% EtOAc/hexanes+2% AcOH)