反应详情

温度

110 °C

A suspension of 1-cyclobutyl-4-(4-iodophenoxy)piperidine (3 g; can be synthesized in accordance with the method described in WO2008072703), methyl 1H-pyrrole-3-carboxylic acid (1.75 g), N,N′-dimethylethylenediamine (0.592 g), copper iodide (0.32 g) and cesium carbonate (2.32 g) in toluene (8.4 mL) was stirred at 110° C. for 4 hours. The reaction mixture was left to cool to room temperature and, after adding chloroform, filtered through Celite (registered trademark). The filtrate was concentrated under reduced pressure and the resulting residue was purified by silica gel column chromatography (NH form silica gel; eluent: n-hexane/ethyl acetate=88/12-0/100) to give the titled compound as a colorless solid (1.42 g).

1. customcan be synthesized in accordance with the method
2. waitThe reaction mixture was left
3. temperatureto cool to room temperature
4. filtrationfiltered through Celite (registered trademark)
5. concentrationThe filtrate was concentrated under reduced pressure
6. customthe resulting residue was purified by silica gel column chromatography (NH form silica gel; eluent: n-hexane/ethyl acetate=88/12-0/100)