反应详情

A solution of 5-bromo-2-(2-cyclohexyl-vinyl)-1H-benzimidazole (1.2 g, 3.9 mmol, prepared as in STEP B above), 2-trifluoromethoxyphenylboronic acid (1.6 g, 7.8 mmol), dichloro[1,1′-bis(diphenylphosphino)ferrocene]palladium (II) dichloromethane adduct (0.752 g, 0.92 mmol) in dimethoxyethane (32 mL) and 2M sodium carbonate (16 mL, 32 mmol) was stirred at 95° C. for 18 h. The resulting solution was cooled to room temperature and poured into a mixture of ethyl acetate and water (1:1, 50 mL). The layers were separated and the organic layer was washed with brine, dried over sodium sulfate, filtered and concentrated. The residue was purified on silica using 3:7 v/v ethyl acetate/hexanes to yield 2-(2-cyclohexyl-vinyl)-5-(2-trifluoromethoxy-phenyl)-1H-benzimidazole.

1. customThe layers were separated
2. washthe organic layer was washed with brine
3. dry with materialdried over sodium sulfate
4. filtrationfiltered
5. concentrationconcentrated
6. customThe residue was purified on silica using 3:7 v/v ethyl acetate/hexanes