Hydrochloric Acid → HCID 71736742, compound

Participants

Reaction Steps

To a mixture of 1-cyano-4-hydroxy-7-phenoxy-isoquinoline-3-carboxylic acid methyl ester (50 mg, 0.16 mmol) and 3-amino-2-(R)-methyl-propionic acid, trifluoroacetic acid salt (32 mg, 0.32 mmol) was added 0.5 M NaOMe/MeOH solution (1.52 mL) (to bring the pH of the mixture to 8). The resultant mixture was microwaved at 130° C. for 1 h. Reaction mixture was diluted with water (80 mL) and acidified by 1 N HCl to pH=3-4. It was extracted with EtOAc. Organic layer was washed with brine, dried over MgSO4, filtered and concentrated. Crude product was purified by silica gel chromatography, eluting with 5-100% EtOAc/CH2Cl2, to provide the title compound 8.6 mg (0.022 mmol) in 14% yield. LC-MS ESI−: 390.12 (M−1)−.

Provenance & Evidence