反应详情

温度

110 °C

4-Bromo-1-(4-fluorophenyl)indazole (291 mg, 1 mmol), copper(I)iodide (9.5 mg, 0.05 mmol), sodium iodide (300 mg, 2 mmol) and (1R,2R)—(N,N′-dimethylcyclohexane-1,2-diamine (14.2 mg, 0.1 mmol) in dioxane (1 ml) were mixed and stirred in argon at 110° C. All starting material was consumed after 24 h. The mixture was cooled and ammonia (5 ml, 28% in water) and water (20 ml) were added followed by extraction with DCM (2×15 ml). The organic phase was concentrated and the crude product was purified by flash chromatography (EtOAc/Heptane) to give the title compound (322 mg, 98%).

1. customwas consumed after 24 h
2. temperatureThe mixture was cooled
3. additionammonia (5 ml, 28% in water) and water (20 ml) were added
4. extractionfollowed by extraction with DCM (2×15 ml)
5. concentrationThe organic phase was concentrated
6. customthe crude product was purified by flash chromatography (EtOAc/Heptane)