反应详情

温度

110 °C

A suspension of 6-chloro-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-pyrazolo[4,3-c]pyridine (1.30 g, 4.6 mmol), 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (1.16 g, 6 mmol), and Pd(dppf)Cl2 (437 mg, 0.6 mmol) in aq. Na2CO3 (2.0 M, 12 mL) and 1,4-dioxane (20 mL) was heated at 110° C. for 20 hours. The reaction mixture was concentrated under reduced pressure. The residue was purified by silica gel chromatography using ethyl acetate/heptanes 50% to 100% as eluting solvents to afford 6-(1H-pyrazol-4-yl)-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-pyrazolo[4,3-c]pyridine as a yellow oil (670 mg, 46%), and recovered 1 g of the starting material. MS (ESI) m/z: 316 [M+H]+.

1. concentrationThe reaction mixture was concentrated under reduced pressure
2. customThe residue was purified by silica gel chromatography
3. washas eluting solvents