反应详情

温度

90 °C

6-(6-Chloro-imidazo[1,2-b]pyridazin-3-ylmethyl)-5,7-difluoro-quinoline (Stage 171.2, 100 mg, 0.299 mmol) was dissolved in DME (3 mL) under argon atm. 4-(4,4,5,5-Tetramethyl-[1,3,2]dioxaborolan-2-yl)-pyrazole-1-carboxylic acid tert-butyl ester (136 mg, 0.449 mmol) was added, followed by 2 M K2CO3 (0.40 mL) and PdCl2(PPh3)2 (10.5 mg, 0.015 mmol). The RM was stirred at 90° C. for 11 h. It was then taken into a mixture of EtOAc and brine and extracted. The combined organic phase was dried on Na2SO4. After evaporation of the solvent the crude was purified by flash chromatography in silica gel with the eluent DCM/MeOH=10:1. The collected fractions containing product were concentrated, dried under vacuo. The title compound was obtained as a white solid (tR 2.97 min (conditions 13), MH+=363).

1. extractionextracted
2. customThe combined organic phase was dried on Na2SO4
3. customAfter evaporation of the solvent the crude
4. customwas purified by flash chromatography in silica gel with the eluent DCM/MeOH=10:1
5. additionThe collected fractions containing product
6. concentrationwere concentrated
7. customdried under vacuo