反応 #45934

反応方程式

4-(4-fluoro-3-trifluoromethyl-phenoxy)-aniline

DMF

alpha-bromoacetophenone

→

desired product

4-(4-{2-butyl-1-[4-(4-fluoro-3-trifluoromethyl-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-1-methyl-piperidine

溶媒

H2O

Et2O

反応条件

後処理

1. 1
   洗浄The combined organic layers were washed with brine
2. 2
   乾燥dried over sodium sulfate
3. 3
   その他Evaporation of solvent in vacuuo

実験手順

To a stirred solution of 4-(4-fluoro-3-trifluoromethyl-phenoxy)-aniline (1.64 mmol) in anhydrous DMF (30 mL) DIEA (3 eq) was added, followed by slow addition of the alpha-bromoacetophenone described above (2 eq), according to General Procedure R2. The reaction mixture was stirred under nitrogen at rt until completion, as indicated by TLC and HPLC. The reaction mixture was then diluted with cold H2O and the product was isolated in Et2O. The combined organic layers were washed with brine and dried over sodium sulfate. Evaporation of solvent in vacuuo afforded the desired product. The crude alkylated aniline was purified by chromatography on silica gel (elution with 5-20% EtOAc/Hexane).

出典