反应详情

1-(4-Fluoro-phenyl)-1H-indazole-4-carboxylic acid (6-trimethylsilanylethynyl-pyridin-3-ylmethyl)-amide (70.0 mg, 0.158 mmol) was dissolved in THF (1.0 mL) and treated with a 1 M solution of TBAF in THF (0.16 mL, 0.16 mmol) at room temperature. The solution was stirred for 2 hours and then diluted with diethyl ether (10 mL) and quenched with water (10 mL). The aqueous layers were extracted with diethyl ether (3×5 mL). The combined organic layers were washed with brine (10 mL), dried over MgSO4 and concentrated. The crude product was purified by silica gel chromatography eluting with a gradient of 0-70% ethyl acetate in hexanes to afford the title compound as a white solid.

1. customquenched with water (10 mL)
2. extractionThe aqueous layers were extracted with diethyl ether (3×5 mL)
3. washThe combined organic layers were washed with brine (10 mL)
4. dry with materialdried over MgSO4
5. concentrationconcentrated
6. customThe crude product was purified by silica gel chromatography
7. washeluting with a gradient of 0-70% ethyl acetate in hexanes