反应详情

温度

100 °C

A mixture of 2,4-dichloropyrimidine (1.00 g, 6.71 mmol), tert-butyl 4-(cyanomethyl)-4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate (2.8 g, 6.7 mol), tetrakis(triphenylphosphine)palladium (0.5 g, 0.4 mmol), and potassium phosphate (4.3 g, 20 mmol) in 1,4-dioxane (20 mL) and water (2 mL) was heated at 100° C. overnight. After cooling to room temperature, the mixture was diluted with EtOAc, washed with water, brine, dried over MgSO4, and concentrated. The residue was purified on silica gel, eluting with 0 to 100% EtOAc in hexanes, to give the desired product (2.19 g, 82%). LCMS (M+H) 403.0.

1. temperatureAfter cooling to room temperature
2. washwashed with water, brine
3. dry with materialdried over MgSO4
4. concentrationconcentrated
5. customThe residue was purified on silica gel
6. washeluting with 0 to 100% EtOAc in hexanes