反应详情

A mixture of 1-cyano-4-hydroxy-7-(4-fluoro-2-chloro-phenoxy)-isoquinoline-3-carboxylic acid ethyl ester (50 mg, 0.13 mmol) and 5-amino-petanoic acid (45 mg, 0.39 mmol) in 0.5 M NaOMe/MeOH solution was microwaved at 130° C. for 1 h. Reaction mixture was diluted with water (60 mL) and acidified by 1 N HCl to pH=3-4. Precipitate was collected and dried. Crude product was then purified by silica gel chromatography, eluting with 5-70% EtOAc/hexanes to provide the title compound 27 mg (0.06 mmol) in 45% yield. LC-MS ESI−: 455.89 (M−1)−.

1. customwas microwaved at 130° C. for 1 h
2. customReaction mixture
3. customPrecipitate was collected
4. customdried
5. customCrude product was then purified by silica gel chromatography
6. washeluting with 5-70% EtOAc/hexanes