1-Methyl-3-(trifluoroacetyl)-1H-indole → 1-(4-Fluorophenyl)-5-[2,2,2-trifluoro-1-hydroxy-1-(1-methyl-1H-indol-3-yl)ethyl]-1,3-dihydrobenzimidazol-2-one

関与物質

反応手順

To a chilled (−78° C.) solution of 5-bromo-1-(4-fluorophenyl)-1,3-dihydrobenzimidazol-2-one (152 mg, 0.5 mmol) in anhydrous bis(2-methoxyethyl)ether (10 mL) was added 0.5 mL (1.25 mmol) of a solution of 2.5 M n-butyllithium in hexanes. After 30 minutes, a solution of 2,2,2-trifluoro-1-(1-methyl-1H-indol-3-yl)ethanone (114 mg) in bis(2-methoxyethyl) in 1 mL of ether was added. The mixture stirred for 1 hour and was quenched with ammonium chloride solution. The resulting precipitate was filtered, washed with water, and dried to afford the title compound as an off-white solid. MS m/z 456 (MH+).

情報源と証拠