反应详情

温度

60 °C

Ethynyl(trimethyl)silane (432 mg, 4.4 mmol), copper iodide(76 mg, 0.4 mmol), triethylamine (2.02 g, 20 mmol) and palladium tetrakis triphenylphosphine (231 mg, 0.2 mmol) were added to a solution of (5R)-3-(3-fluoro-4-iodophenyl)-5-[(4-methyl-1H-1,2,3-triazol-1-yl)methyl]-1,3-oxazolidin-2-one (WO2003072575) (Intermediate 2,1.61 g, 4.0 mmol) in a sealed reaction vessel. The reaction mixture was stirred at 60° C. over night, then cooled down to room temperature and filtered through celite. The filtrate was concentrated and purified by flash chromatography on silica gel with 30% hexanes in ethyl acetate. The product was obtained as a yellowish solid (1.4 g).

1. temperaturecooled down to room temperature
2. filtrationfiltered through celite
3. concentrationThe filtrate was concentrated
4. custompurified by flash chromatography on silica gel with 30% hexanes in ethyl acetate