Ethyl Acetate → 6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-amine

関与物質

反応手順

3-Amino-6-chloropyridazine (7.76 g, 59.9 mmol) was introduced in a round bottom flask with 1-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaboran-2-yl)-1H-pyrazole (13.1 g, 59.9 mmol) and dissolved in 2-dimethoxyethane (160 mL). An aqueous solution of 2 M Na2CO3 (110 mL, 220 mmol) was added to this mixture and also tetrakis-(triphenylphosphine)-palladium (3.5 g, 2.99 mmol). The RM was refluxed for 26 h under nitrogen. Then was taken up with EtOAc and washed with 1N NaOH and brine. The organic layer was dried over Na2SO4 and the solvent was removed. The residue was triturated with Et2O to afford the title compound as a yellow solid (tR 0.9 min (conditions 2), MH+=176).

情報源と証拠