反应详情

To 4-[3-(4-Benzyloxy-2-fluoro-phenyl)-1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-4-yl]-pyridine (900 mg) was added trifluoroacetic acid (5.25 ml) and anisole (1.15 ml) and the reaction mixture heated at reflux for 18 h. The reaction mixture was quenched with with 1N NaOH, extracted 3× tetrahydrofuran, dried magnesium sulfate, filtered and concentrated. Purification via Biotage MPLC eluting with 5% methanol/1% ammonium hydroxide/ethyl acetate provided the title compound (552 mg). MS: (M+H m/z=338.2).

1. temperaturethe reaction mixture heated
2. temperatureat reflux for 18 h
3. customThe reaction mixture was quenched with with 1N NaOH
4. extractionextracted 3× tetrahydrofuran, dried magnesium sulfate
5. filtrationfiltered
6. concentrationconcentrated
7. customPurification via Biotage MPLC
8. washeluting with 5% methanol/1% ammonium hydroxide/ethyl acetate