反应详情

温度

80 °C

A mixture of methyl[3-fluoro-6-(methyloxy)-1,5-naphthyridin-4-yl]acetate (35.79 g, 143 mmol), benzyltriethylammonium chloride (51.5 g), potassium carbonate (30.4 g) and paraformaldehyde (30.4 g) in cyclohexane (1 litre) was stirred at 80° C. under argon overnight, cooled and shaken with water and ethyl acetate. After separation, the aqueous was re-extracted with ethyl acetate and the combined organic phases dried and evaporated. Chromatography, eluting with 15% ethyl acetate/hexane, provided the product (24.66 g, 66%).

1. temperaturecooled
2. customAfter separation
3. extractionthe aqueous was re-extracted with ethyl acetate
4. customthe combined organic phases dried
5. customevaporated
6. washChromatography, eluting with 15% ethyl acetate/hexane