反应详情

温度

95 °C

To 3-(4-(7-chloroimidazo[1,2-c]pyrimidin-5-yl)-1H-pyrazol-1-yl)-3-cyclopropyl-propanenitrile (Preparation M; 100 mg, 0.320 mmol) in dioxane (10 mL) was added K2CO3 (88.4 mg, 0.639 mmol), diacetoxypalladium (7.18 mg, 0.0320 mmol), triphenylphosphine (16.8 mg, 0.0639 mmol) and tert-butyl 5,6-dihydroimidazo[1,2-a]pyrazine-7(8H)-carboxylate (107 mg, 0.480 mmol). The reaction was sealed and heated to 95° C. for 5 hours. The reaction was cooled to ambient temperature and concentrated under reduced pressure. The residue was purified by silica gel chromatography (DCM/MeOH/NH4OH 10:1:0.1) to give the final product (33 mg, 26% yield). MS (apci) m/z=400.4 (M+H).

1. customThe reaction was sealed
2. temperatureThe reaction was cooled to ambient temperature
3. concentrationconcentrated under reduced pressure
4. customThe residue was purified by silica gel chromatography (DCM/MeOH/NH4OH 10:1:0.1)