反应详情

温度

100 °C

To a suspension of 6-(pyridin-3-yl)pyrrolo[2,1-f][1,2,4]triazin-4-ol (100 mg, 0.30 mmol) in 10 mL of toluene were added POCl3 (0.18 mL, 1.88 mmol) and DIEA (0.09 mL, 0.5 mmol). The suspension was heated at 100° C. for 7 h. After cooling down, the excess POCl3 was removed under reduced pressure. The residue was suspended in EtOAc, and then neutralized with sat. NaHCO3. The organic layer was then washed with brine and dried over MgSO4. After filtration and concentration, the residue was purified by flash column chromatography to afford the title compound (23 mg, 33%). MS(ESI+) m/z 231.2/233.2 (M+H)+.

1. temperatureAfter cooling down
2. customthe excess POCl3 was removed under reduced pressure
3. washThe organic layer was then washed with brine
4. dry with materialdried over MgSO4
5. filtrationAfter filtration and concentration
6. customthe residue was purified by flash column chromatography