反应详情

1.80 g (3.18 mmol) of tert-butyl 1-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}benzyl)-2,2-difluorocyclopropanecarboxylate (as diastereomer mixture) were dissolved in 5 ml of dichloromethane, and 4.9 ml of TFA were added at RT. The reaction mixture was stirred at RT for 1 h and then concentrated under reduced pressure. The residue was purified by chromatography on silica gel (mobile phase first dichloromethane, then dichloromethane/ethyl acetate 10:1→5:1). This gave 1.25 g of the target compound (77.1% of theory).

1. concentrationconcentrated under reduced pressure
2. customThe residue was purified by chromatography on silica gel (mobile phase first dichloromethane