反应详情

To a stirred solution of 2-(4-(1-(tert-butyldimethylsilyloxy)cyclopropyl)-3-fluorophenyl)-N-((1-(3-chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-5-yl)methyl)-propanamide (103 mg, 0.173 mmol, 1 eq) in THF (5 mL) was added TBAF (90 mg, 0.346 mmol, 2 eq) at room temperature and the mixture was stirred for 2 h after which THF was evaporated and the residue was dissolved in ethyl acetate (15 mL), washed with water (10 mL×2), brine (10 mL) and the solvent evaporated. The residue was purified by CC using methanol/CHCl3 (1:9) as eluent to give N-((1-(3-chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-5-yl)methyl)-2-(3-fluoro-4-(1-hydroxycyclopropyl)phenyl)propanamide (41 mg, 49%) as off white solid (TLC system: methanol/CHCl3 (1:9) Rf: 0.5).

1. customwas evaporated
2. dissolutionthe residue was dissolved in ethyl acetate (15 mL)
3. washwashed with water (10 mL×2), brine (10 mL)
4. customthe solvent evaporated
5. customThe residue was purified by CC