反应详情

温度

-78 °C

DAST (19 μL, 0.15 mmol) was added dropwise to a solution of 4-pyridin-2-yl-1-quinoxalin-2-yl-but-3-yn-1-ol (30 mg, 0.11 mmol) in DCM (1.5 mL) at −78° C. The reaction mixture was stirred for 15 min at −78° C., quenched by the addition of water at 0° C. and extracted twice with DCM. The organic phase was washed with water, dried over Na2SO4, filtered and evaporated. The crude residue was purified by flash chromatography (cyclohexane/AcOEt 1:1) to yield 10 mg (36 μmol, 33%) of 2-(1-fluoro-4-(pyridin-2-yl)but-3-ynyl)quinoxaline as an orange semi-solid with a purity of 70%.

1. customquenched by the addition of water at 0° C.
2. extractionextracted twice with DCM
3. washThe organic phase was washed with water
4. dry with materialdried over Na2SO4
5. filtrationfiltered
6. customevaporated
7. customThe crude residue was purified by flash chromatography (cyclohexane/AcOEt 1:1)