Реакция #62181

Уравнение реакции

4-[3-(4-Benzyloxy-2-fluoro-phenyl)-1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-4-yl]-pyridine

trifluoroacetic acid

anisole

→

title compound

Выход 77.7%

3-Fluoro-4-[4-pyridin-4-yl-1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-phenol

Выход 77.7%

Условия реакции

Обработка

1. 1
   Температураthe reaction mixture heated
2. 2
   Температураat reflux for 18 h
3. 3
   ДругоеThe reaction mixture was quenched with with 1N NaOH
4. 4
   Экстракцияextracted 3× tetrahydrofuran, dried magnesium sulfate
5. 5
   Фильтрацияfiltered
6. 6
   Концентрированиеconcentrated
7. 7
   ДругоеPurification via Biotage MPLC
8. 8
   Промывкаeluting with 5% methanol/1% ammonium hydroxide/ethyl acetate

Методика

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).

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