反应详情

To a mixture of 1-cyano-7-cyclohexanesulfonyl-4-hydroxy-isoquinoline-3-carboxylic acid butyl ester (30 mg, 0.072 mmol) and 1-aminomethyl-cyclobutanecarboxylic acid (48 mg, 0.29 mmol) (available from Ukrorgsyntez Ltd) in ethanol (0.7 mL) was added NaOMe solid (16 mg, 0.29 mmol). The resultant mixture was microwaved at 140° C. for 1 h. The reaction mixture was then treated with 1 mL of 3 N NaOH aqueous solution and stirred at room temperature for 3 h. Reaction mixture was diluted with water (60 mL) and acidified by 1 N HCl to pH=3-4. Precipitate was collected and purified by silica gel chromatography, eluting with 0-10% MeOH/CH2Cl2 to provide the title compound 6.4 mg (0.014 mmol) in 19% yield. LC-MS ESI−: 470.12 (M−1)−.

1. customReaction mixture
2. customPrecipitate was collected
3. custompurified by silica gel chromatography
4. washeluting with 0-10% MeOH/CH2Cl2