反应详情

A suspension of tert-butyl 4-(6-(6-chloro-1H-pyrazolo[4,3-c]pyridin-1-yl)pyrazin-2-yl)-1,4-diazepane-1-carboxylate (400 mg, 0.93 mmol), 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (271 mg, 1.4 mmol), Pd(dppf)Cl2 (81 mg, 0.093 mmol) and a solution of Na2CO3 (2.0 M, 1.5 mL) in 1,4-dioxane (6 mL) under argon in a sealed vial was heated at 120° C. for 1 hour. The reaction mixture was filtered and the filtrate was concentrated under reduced pressure to give a residue. The residue was purified by silica gel chromatography using petroleum ether/ethyl acetate (10% to 60%) as eluting solvents to afford tert-butyl 4-(6-(6-(1H-pyrazol-4-yl)-1H-pyrazolo[4,3-c]pyridin-1-yl)pyrazin-2-yl)-1,4-diazepane-1-carboxylate as yellow solid (180 mg, 42%). MS (ESI) m/z: 462 [M+H]+.

1. filtrationThe reaction mixture was filtered
2. concentrationthe filtrate was concentrated under reduced pressure
3. customto give a residue
4. customThe residue was purified by silica gel chromatography
5. washas eluting solvents