反应详情

A mixture of 7-benzyl-4-hydroxy-8-oxo-1-phenyl-7,8-dihydro-[2,7]naphthyridine-3-carboxylic acid methyl ester (29 mg, 0.075 mmol), glycine (750 mg, 10 mmol) and NaOMe solution (15 mL, 7.5 mmol, 0.5 M in MeOH) was refluxed for 16 h. After the mixture was cooled to r.t., solvent was evaporated in vacuo. 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 was chromatographed (5-70% EtOAc/hexanes+2% AcOH) to give 24 mg of the title compound as a pale yellow solid. MS: (+) m/z 429.99 (M+1).

1. temperaturewas refluxed for 16 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 was chromatographed (5-70% EtOAc/hexanes+2% AcOH)