反应详情

温度

100 °C

The mixture of 5-iodo-3-(pyridin-4-yl)-1-trityl-1H-indazole (281 mg, 0.5 mmol), tert-butyl 3-(1H-pyrazol-3-yl)piperidine-1-carboxylate (151 mg, 0.6 mmol), copper (I) iodide (19 mg, 0.1 mmol), rac-trans-N,N-dimethylcyclohexane-1,2-diamine (57 mg, 0.4 mmol), K2CO3 (552 mg, 4 mmol) in toluene (3 mL) was heated at 100° C. for 4 days. After cooling to room temperature, the reaction mixture was filtered through a pad of celite, and washed with EtOAc. The filtrate was concentrated and column purified with mixture of methanol, dichloromethane and ammonia to give tert-butyl 3-(1-(3-(pyridin-4-yl)-1-trityl-1H-indazol-5-yl)-1H-pyrazol-3-yl)piperidine-1-carboxylate (380 mg).

1. temperatureAfter cooling to room temperature
2. filtrationthe reaction mixture was filtered through a pad of celite
3. washwashed with EtOAc
4. concentrationThe filtrate was concentrated
5. customcolumn purified with mixture of methanol, dichloromethane and ammonia