反应详情

温度

-78 °C

n-Butyl lithium (2.5 M in hexane, 11 mmol, 4.83 mL) was added dropwise over 15 minutes to a solution of 5-fluoro-3-methyl benzofuran (11 mmol, 1.65 mg) in THF (20 mL) cooled to −78° C. To this was added 3-fluorosulfonyl-6-methoxy-pyridazine (11 mmol, 2.11 g) and stirred for 30 minutes. The reaction mixture was allowed to come to room temperature overnight and was then quenched with EtOAc (40 mL) and H2O (10 mL). The organic portion was collected, dried, filtered and the filtrate was evaporated to dryness to obtain a crude product, which was purified by silica gel chromatography (eluent:hexanes:EtOAc::4:1) to obtain the desired product: 3-methoxy-6-(5-fluoro-3-methyl-benzofuran-2-sulfonyl)-pyridazine (22%, 781 mg).

1. waitto come to room temperature overnight
2. customwas then quenched with EtOAc (40 mL) and H2O (10 mL)
3. customThe organic portion was collected
4. customdried
5. filtrationfiltered
6. customthe filtrate was evaporated to dryness
7. customto obtain a crude product, which
8. customwas purified by silica gel chromatography (eluent:hexanes:EtOAc::4:1)