反应详情

A mixture of 4-hydroxy-7-(4-methoxy-phenoxy)-isoquinoline-3-carboxylic acid methyl ester (100 mg, 0.31 mmol) and 3-amino-2-(S)-hydroxy-propionic acid (97 mg, 0.92 mmol) in 0.5 M NaOMe/MeOH solution (1.23 mL, 0.62 mmol) was microwaved at 120° C. for 2 h. After cooled, solid precipitate was collected and rinsed with cold MeOH (1 mL). Solid was dissolved in water (40 mL), acidified by 1 N HCl to pH=3-4 and extracted with EtOAc. Organic layer was dried over MgSO4, filtered and concentrated to provide the title compound 54 mg (0.14 mmol) in 15% yield. LC-MS ESI−: 397.02 (M−1)−.

1. customwas microwaved at 120° C. for 2 h
2. temperatureAfter cooled
3. customsolid precipitate was collected
4. washrinsed with cold MeOH (1 mL)
5. dissolutionSolid was dissolved in water (40 mL)
6. extractionextracted with EtOAc
7. dry with materialOrganic layer was dried over MgSO4
8. filtrationfiltered
9. concentrationconcentrated