反应详情

温度

80 °C

To a solution of tert-butyl 5-(trifluoromethylsulfonyloxy)-3,4-dihydropyridine-1(2H)-carboxylate (2.0 g, 6.0 mmol) in dioxane (40 mL) was added 1-methyl-1H-pyrazol-5-ylboronic acid (0.83 g, 6.60 mmol), Na2CO3 (1.90 g, 18.1 mmol), and Pd(dppf)Cl2 (370 mg, 0.600 mmol). The resulting mixture was stirred at 80° C. for 18 h. After concentration, the residue was purified by silica gel chromatography eluting with a 0-25% gradient of EtOAc in petroleum ether to give tert-butyl 5-(1-methyl-1H-pyrazol-5-yl)-3,4-dihydropyridine-1(2H)-carboxylate (0.80 g, 58% yield) as pale yellow oil. LCMS (ESI) m/z: 263.2 [M+H+].

1. concentrationAfter concentration
2. customthe residue was purified by silica gel chromatography
3. washeluting with a 0-25% gradient of EtOAc in petroleum ether