反应详情

A solution of 5-bromomethyl-1H-indazole hydrobromide salt (194 mg, 0.665 mmol) and 3,4-dihydro-2H-pyran (0.118 mL, 1.29 mmol) in tetrahydrofuran (4.7 mL) was heated at reflux for 2 h and then stirred overnight at room temperature. Dichloromethane (12 mL) was added and the solution was washed with aqueous sodium hydrogen carbonate, water, and brine (10 mL each), dried (MgSO4), concentrated, and chromatographed (5–60% ethyl acetate/petroleum ether) to give 4-bromomethyl-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole (153 mg, 78%) as an off-white solid.

1. temperatureat reflux for 2 h
2. washthe solution was washed with aqueous sodium hydrogen carbonate, water, and brine (10 mL each)
3. dry with materialdried (MgSO4)
4. concentrationconcentrated
5. customchromatographed (5–60% ethyl acetate/petroleum ether)