反应详情

温度

140 °C

A mixture of 1-benzyl-5-hydroxy-2-oxo-3-phenyl-8-pyridin-3-yl-1,2-dihydro-[1,7]naphthyridine-6-carboxylic acid methyl ester (38.5 mg, 0.083 mmol), N-(2-amino-ethyl)-N-methyl-methanesulfonamide HCl salt (78 mg, 0.42 mmol), and NaOMe (22 mg, 0.42 mmol) in EtOH (3 mL) was heated at 140° C. for 6 h in a microwave reactor. Solvent was evaporated in vacuo, and the residue was partitioned between EtOAc and water. 1 M HCl was added until pH was about 3. The aqueous layer was extracted with additional EtOAc, and the combined organic layer was dried over MgSO4 and concentrated. The residue was purified by silica gel chromatography (0-10% MeOH/CH2Cl2) to give 26 mg of the title compound. MS: (+) m/z 584.26 (M+1).

1. customSolvent was evaporated in vacuo
2. customthe residue was partitioned between EtOAc and water
3. addition1 M HCl was added until pH was about 3
4. extractionThe aqueous layer was extracted with additional EtOAc
5. dry with materialthe combined organic layer was dried over MgSO4
6. concentrationconcentrated
7. customThe residue was purified by silica gel chromatography (0-10% MeOH/CH2Cl2)