反应详情

温度

150 °C

A microwave tube was charged with rac-(6-Chloro-imidazo[1,2-b]pyridazin-3-yl)-quinolin-6-ylmethanol (Stage 1.1, 1.12 g, 3.60 mmol), 1-methyl-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1H-pyrazole (789 mg, 3.60 mmol), tetrakis-(triphenylphosphine)palladium (210 mg), 2M Na2CO3 (6.5 mL) and DME (11 mL). It was heated at 150° C. under microwave irradiation for 10 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 reside was purified by MPLC eluting with a DCM/MeOH gradient to afford the title compound as a brown solid (tR 1.0 min(conditions 1), MH+=357).

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 reside was purified by MPLC
6. washeluting with a DCM/MeOH gradient