反应详情

温度

145 °C

4-[2-(2,4-Dichloro-phenyl)-1-hydroxy-1-trifluoromethyl-propyl]-1H-pyridin-2-one (Example 119, 158 mg) was dissolved in toluene (5 mL), and treated with bromo-acetic acid methyl ester (0.03 mL) and silver carbonate (53 mg). The reaction mixture was then stirred at 145° C. (Bath-temperature) for 3.5 h, cooled down to r.t., filtered-off and concentrated in vacuo. The residue was purified by flash chromatography (10 g silica gel, ethyl acetate/heptane 1:9) to give the title compound as colorless oil (30 mg). MS (m/e)=438.3 (MH+).

1. temperaturecooled down to r.t.
2. concentrationfiltered-off and concentrated in vacuo
3. customThe residue was purified by flash chromatography (10 g silica gel, ethyl acetate/heptane 1:9)