反应详情

To a suspension of 4-hydroxy-3-[1-oxo-3-(pyridin-4-yl)propyl]-1-phenyl-1,8-naphthyridin-2 (1H)-one (100 mg, 0.27 mmol, prepared in Synthetic Example 1) in ethanol (2 ml) was added methylhydrazine (40 μl, 0.75 mmol, 2.8 eq.) and the mixture was stirred at room temperature to form a solution which was then stirred for 30 minutes. After it was perceived that precipitation started, the mixture was heated under reflux for 3 hours and cooled to room temperature. Next, to the liquid mixture was added additional methylhydrazine (40 μl, 0.75 mmol, 2.8 eq.) and the resultant mixture was heated overnight with stirring at 70° C. The liquid reaction mixture was cooled to room temperature, and then filtered to give precipitates which were dried to obtain 1-methyl-5-phenyl-3-[2-(pyridin-4-yl)ethyl]-1H-pyrazolo[4,3-c][1,8]naphthyridin-4 (5H)-one (94 mg, 92%).

1. customto form a solution which
2. stirringwas then stirred for 30 minutes
3. customAfter it was perceived that precipitation
4. temperaturethe mixture was heated
5. temperatureunder reflux for 3 hours
6. temperaturecooled to room temperature
7. stirringwith stirring at 70° C
8. customThe liquid reaction mixture
9. temperaturewas cooled to room temperature
10. filtrationfiltered
11. customto give
12. customprecipitates which
13. customwere dried