反应详情

温度

110 °C

A mixture of 4-bromo-7-chloro-6-azaindole (6 g), CuBr (3.7 g) and NaOMe (30 mL, 5% in MeOH) was heated at 110° C. for 24 hours in a sealed tube. After cooling to room temperature, the reaction mixture was added to saturated aqueous NH4Cl. The resulting aqueous solution was extracted with EtOAc (3×30 mL). The combined organic layer was dried over MgSO4, filtered and the filtrate was concentrated in vacuo to afford a residue, which was purified by using silica gel chromatography to give 1.8 g of 4-methoxy-7-chloro-6-azaindole, Precursor 2e.

1. temperatureAfter cooling to room temperature
2. extractionThe resulting aqueous solution was extracted with EtOAc (3×30 mL)
3. dry with materialThe combined organic layer was dried over MgSO4
4. filtrationfiltered
5. concentrationthe filtrate was concentrated in vacuo
6. customto afford a residue, which
7. customwas purified