反应详情

A mixture of 4-hydroxy-7-phenoxy-isoquinoline-3-carboxylic acid methyl ester (90 mg, 0.31 mmol) and 2-(S)-hydroxy-3-amino-propionic acid (Sigma-Aldrich) (96 mg, 0.92 mmol) in 0.5 N NaOMe in MeOH solution (1.22 mL, 0.61 mmol) was microwaved at 120° C. for 1 h and concentrated. Residue was dissolved in water (70 mL) and acidified by 1 N HCl solution to pH=3-4. It was extracted with EtOAc, Organic layer was washed with brine, dried over MgSO4, filtered and concentrated to give the title compound (105 mg, 0.29 mmol) in 92% yield. LC-MS ESI−: 366.99 (M−1)−.

1. customwas microwaved at 120° C. for 1 h
2. concentrationconcentrated
3. dissolutionResidue was dissolved in water (70 mL)
4. extractionIt was extracted with EtOAc, Organic layer
5. washwas washed with brine
6. dry with materialdried over MgSO4
7. filtrationfiltered
8. concentrationconcentrated