反应详情

1-{4-[5-(4-fluorophenyl)pyrimidin-2-yl]piperazine-1-sulfonylmethyl}cyclohexanecarboxylic acid methyl ester (0.40 g) and lithium hydroxide monohydrate (0.20 g) were combined in tetrahydrofuran (20 ml), methanol (10 ml) and water (5 ml) and heated to reflux for 10 h. The organic solvents were then removed under reduced pressure. The aqueous residue was diluted with water (20 ml), acidified with citric acid to approximately pH 4, and a white precipitate filtered off. After drying the precipitated solid was triturated with hot ethyl acetate (30 ml) to provide the title compound as a white solid (0.27 g, 69%).

1. temperatureto reflux for 10 h
2. customThe organic solvents were then removed under reduced pressure
3. additionThe aqueous residue was diluted with water (20 ml)
4. filtrationa white precipitate filtered off
5. customAfter drying the precipitated solid
6. customwas triturated with hot ethyl acetate (30 ml)