反应详情

温度

85 °C

A mixture of Example 7a (1.44 g, 3.57 mmol), acetamide (0.295 g, 4.99 mmol), cesium carbonate (1.743 g, 5.35 mmol), palladium (II) acetate (0.024 g, 0.107 mmol), and Xantphos (0.093 g, 0.161 mmol) was degassed and heated at 85° C. in a sealed vial for 6 hours. The reaction mixture was cooled and concentrated. The residue was treated with 20% brine and extracted with EtOAc (2×). The organic layers were dried, concentrated, and purified on a 40 g column using the ISCO Companion flash system eluting with CH2Cl2/EtOAc (90:10) to give 0.384 g of the title compound.

1. temperatureThe reaction mixture was cooled
2. concentrationconcentrated
3. additionThe residue was treated with 20% brine
4. extractionextracted with EtOAc (2×)
5. customThe organic layers were dried
6. concentrationconcentrated
7. custompurified on a 40 g column
8. washeluting with CH2Cl2/EtOAc (90:10)