反应详情

A solution of 50 mg (0.143 mmol) C-[2-(4-Isopropyl-phenyl)-7-methoxy-1-(2-methoxy-ethyl)-1H-benzoimidazol-5-yl]-methylamine, 28 mg (0.143 mmol) ethyl-4-bromobutyrate and 28 μl (0.2 mmol) triethylamine in 4 ml 3-methyl-1-butanol is stirred at reflux temperature for 8 h. Then the reaction mixture is poured on water and extracted (3×) with EtOAc. The combined organic layers are washed with water (2×) and brine, dried over MgSO4, filtered and concentrated in vacuo. The residue is purified by flash-chromatography on silica gel (EtOAc:MeOH=98:2) to afford 20 mg of the title compound as a colorless oil.

1. temperatureat reflux temperature for 8 h
2. additionThen the reaction mixture is poured on water
3. extractionextracted (3×) with EtOAc
4. washThe combined organic layers are washed with water (2×) and brine
5. dry with materialdried over MgSO4
6. filtrationfiltered
7. concentrationconcentrated in vacuo
8. customThe residue is purified by flash-chromatography on silica gel (EtOAc:MeOH=98:2)