反应详情

温度

120 °C

To a solution of 1.03 mmol 4-[5-(2,2-difluoro-vinyl)-thiazol-2-yl]-piperazine-1-carboxylic acid tert-butyl ester in 7.5 dimethylsulphoxide and 0.3 ml water was added 7.18 mmol potassium fluoride and the mixture was heated at 120° C. for 2 h. The mixture was then diluted with ethyl acetate and washed sequentially with water and brine. The organic phase was dried over sodium sulphate and concentrated in vacuo. The residue was purified by chromatography (SiO2, ethyl acetate/heptane) to afford the title compound as a yellow crystalline solid (yield 90%). MS (m/e): 352.3 (M+H+, 100%).

1. washwashed sequentially with water and brine
2. dry with materialThe organic phase was dried over sodium sulphate
3. concentrationconcentrated in vacuo
4. customThe residue was purified by chromatography (SiO2, ethyl acetate/heptane)