反应详情

A solution of [8-fluoro-2-isopropyl-4-methyl-3-(4-pyrazol-1-ylbenzyl)quinolin-5-yloxy]acetic acid methyl ester (0.062 g) in tetrahydrofuran (0.70 mL) and water (0.70 mL) was treated with lithium hydroxide (0.033 g), and the resulting mixture was stirred at room temperature. After 24 hours, the mixture was treated with additional lithium hydroxide (0.033 g) and stirring continued for 16 hours. The mixture was cooled to 0° C., acidified with 1.0 M aqueous hydrochloric acid and extracted with ethyl acetate (3×5.0 mL). The combined extracts were washed with saturated aqueous sodium chloride solution (2.0 mL), dried over magnesium sulfate and concentrated under reduced pressure. Purification of the residue by preparative reverse-phase HPLC, eluting with a mixture of acetonitrile and water (40:60 to 19:1 by volume) gave title compound as a yellow solid (0.015 g).

1. stirringstirring
2. waitcontinued for 16 hours
3. temperatureThe mixture was cooled to 0° C.
4. extractionextracted with ethyl acetate (3×5.0 mL)
5. washThe combined extracts were washed with saturated aqueous sodium chloride solution (2.0 mL)
6. dry with materialdried over magnesium sulfate
7. concentrationconcentrated under reduced pressure
8. customPurification of the residue by preparative reverse-phase HPLC
9. washeluting with a mixture of acetonitrile and water (40:60 to 19:1 by volume)