反应详情

温度

0 °C

454.6 mg (1.42 mMol) 6-(6-Chloropyrimidin-4-yloxy)-isoquinoline-1-carbonyl chloride is dissolved in 10 ml CH2Cl2 and cooled to 0° C. At this temperature 0.46 ml (5.9 mMol) pyridine are added followed by 418.0 mg (1.7 mMol) 5-tert-butyl-2-(4-methoxy-phenyl)-2H-pyrazol-3-ylamine (Step 19.1). The reaction mixture is then allowed to warm to rt and stirred at ambient temperature for 1 h. It is worked up by addition of H2O and CH2Cl2. The organic layer is separated washed with brine and dried. After evaporation of the solvents the crude product is purified by chromatography (combi-flash: 40 g column, hexanes/EtOAc, gradient 0-50% EtOAc) to give the title compound as a yellow solid: m.p.: 156° C.; MS.

1. temperatureto warm to rt
2. customThe organic layer is separated
3. washwashed with brine
4. customdried
5. customAfter evaporation of the solvents the crude product
6. customis purified by chromatography (combi-flash: 40 g column, hexanes/EtOAc, gradient 0-50% EtOAc)