反应详情

温度

150 °C

(rac)-(6-Chloro-imidazo[1,2-b]pyridazin-3-yl)-(5,7-difluoro-quinolin-6-yl)-methanol (Stage 171.3, 1.8 g, 5.19 mmol) was introduced in a microwave reactor together with 1-Methyl-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1H-pyrazole (1.08 g, 5.19 mmol), tetrakis(triphenylphosphine)-palladium (300 mg, 0.26 mmol), 2 M Na2CO3 (9.34 mL) and DME (20 mL). The mixture was heated at 150° C. under microwave irradiation for 50 min. The RM was taken up with EtOAc and washed with 10% Na2CO3 and brine. The organic layer was dried over Na2SO4, filtered and concentrated in vacuo. The residue was triturated with Et2O and the precipitate was filtered off to give the title compound as a black solid (tR 0.8 min (conditions 2), MH+=393)

1. washwashed with 10% Na2CO3 and brine
2. dry with materialThe organic layer was dried over Na2SO4
3. filtrationfiltered
4. concentrationconcentrated in vacuo
5. customThe residue was triturated with Et2O
6. filtrationthe precipitate was filtered off