preparation | sodium hydride (0.12g;3.12mmol;1.5 equivalent) was added to a stirring solution of 4-cyano-2 (1H)-pyridone (0.25g;2.08mmol;1 equivalent) in DMF(5mL), and the resulting mixture was stirred at 0°C for 10 minutes. Methyl iodide (0.4mL;6.25mmol;3 equivalents) was then added to the mixture and the resulting mixture was stirred at 23°C for 2h. Dilute the mixture with water (50mL) and extract the organic components (2 × 200mL) with ethyl acetate. Wash the combined organic layer with water and brine, dry on anhydrous sodium sulfate, filter and remove the solvent in vacuum to obtain the title compound (0.18g,67%). |