反应详情

To a mixture of 3-(4-fluoro-benzoyl)-4-oxo-piperidine-1-carboxylic acid tert-butyl ester (0.20 g, 0.62 mmol) and 2-methyl-pyrrolidine-1-carboxamidine trifluoroacetate (0.14 g, 0.58 mmol) in MeCN (3 mL) was added K2CO3 (0.190 g, 1.4 mmol). The mixture was heated at reflux for 15 h, then cooled to rt, diluted with H2O and extracted with CH2Cl2 (2×). The combined organic extracts were dried and concentrated. The residue was purified by FCC to give the title compound (0.193 g, 81%) as a clear oil. MS (ESI): mass calcd. for C23H23FN4O2, 412.5; m/z found, 413.4 [M+H]+.

1. temperatureThe mixture was heated
2. temperatureat reflux for 15 h
3. extractionextracted with CH2Cl2 (2×)
4. customThe combined organic extracts were dried
5. concentrationconcentrated
6. customThe residue was purified by FCC