反应详情

To a solution of 990 mg 4-Carboxymethoxy-7-methyl-quinoline-2-carboxylic acid ethyl ester in 5 ml DMF were added 945 mg pentafluorophenol and 984 mg EDC. The mixture was stirred under exclusion of moisture until LCMS indicated complete conversion to the corresponding pentafluorophenolester. Tert-Butyl 1-piperazinecarboxylate (437 mg) was mixed with 0.8 ml N-ethylmorpholine and 10 ml DMF and this mixture added dropwise to the solution of the pentafluorophenolester. After 12 h the reaction mixture was diluted with DCM and washed with aqueous LiCl (4%) and saturated aqueous NaHCO3. The crude product obtained after evaporation of the solvent was purified by flash chromatography on silica eluting with ethyl acetate/heptane gradient. Yield: 988 mg.

1. additionthis mixture added dropwise to the solution of the pentafluorophenolester
2. washwashed with aqueous LiCl (4%) and saturated aqueous NaHCO3