Potassium Phosphate, Tribasic → tert-butyl 4-(4-(2-chloropyrimidin-4-yl)-1H-pyrazol-1-yl)-4-(cyanomethyl)piperidine-1-carboxylate

関与物質

反応条件

反応手順

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.

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