反应详情

To a solution of (1H-indazol-5-yl)(phenyl)methanol (1.1 g, 5.0 mmol) in 50 mL of dry THF was added EtN3 (2.8 mL, 20 mmol) and acetic anhydride (1.9 mL, 20 mmol). The reaction was heated at reflux for 12 h. The reaction was quenched with aqueous sodium bicarbonate and extracted 2×EtOAc. The organic layers were dried over MgSO4, filtered, and concentrated. The residue was taken up in toluene and concentrated in vacuo×2 to remove any excess acetic anhydride. Obtained a quantitative yield of (1H-indazol-5-yl)(phenyl)methyl acetate. MS found: (M+H)+=309.

1. temperatureThe reaction was heated
2. temperatureat reflux for 12 h
3. customThe reaction was quenched with aqueous sodium bicarbonate
4. extractionextracted 2×EtOAc
5. dry with materialThe organic layers were dried over MgSO4
6. filtrationfiltered
7. concentrationconcentrated
8. concentrationconcentrated in vacuo×2
9. customto remove any excess acetic anhydride