L-Isoserine → 2-(S)-Hydroxy-3-{[4-hydroxy-7-(4-methoxy-phenoxy)-isoquinoline-3-carbonyl]-amino}-propionic acid

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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)−.

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