Barium hydroxide, monohydrate → (2R,3S)-3-amino-4-(3,5-difluorophenyl)-1-(2-(pent-4-enyl)-5-(trifluoromethyl)-benzylamino)butan-2-ol

関与物質

反応条件

反応手順

Step AM (2): To a solution of benzyl (2S,3R)-1-(3,5-difluorophenyl)-3-hydroxy-4-(2-(pent-4-enyl)-5-(trifluoromethyl)benzylamino)butan-2-ylcarbamate trifluoroacetate salt (88 mg, 0.128 mmol) in DME (9.0 mL) and water (6.0 mL) was added barium hydroxide monohydrate (852 mg, 4.5 mmol). The reaction mixture was stirred at 110° C. in a high pressure vial for 18 h. The reaction mixture was filtered through a pad of celite and the filtrate was concentrated in vacuum. The residue was purified by reverse phase chromatography to give (2R,3S)-3-amino-4-(3,5-difluorophenyl)-1-(2-(pent-4-enyl)-5-(trifluoromethyl)-benzylamino)butan-2-ol double trifluoro-acetate salt (64 mg, 74%) as a colorless oil. LC-MS (M+H)+=443.36.

情報源と証拠