反应详情

To a solution of methyl 3-benzyloxy-5,6-dimethyl-4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine-2-carboxylate (72 mg, 0.219 mmol) in MeOH was added 4-fluorobenzylamine (376 μL, 3.28 mmol). The mixture was heated to reflux overnight and then at 110° C. for 4 hours. The mixture was purified by reverse phase chromatography on a C-18 column using a gradient elution of 95-5% H2O (0.1% TFA)/CH3CN (0.1% TFA), and collection and concentration of the appropriate fractions afforded the amide as a yellow oil. ES MS (M+1)=423.

1. temperatureThe mixture was heated
2. temperatureto reflux overnight
3. customThe mixture was purified by reverse phase chromatography on a C-18 column
4. washa gradient elution of 95-5% H2O (0.1% TFA)/CH3CN (0.1% TFA), and collection and concentration of the appropriate fractions