反应详情

温度

130 °C

A sealed tube containing trans-4-(2-amino-5-bromo-6-methylpyrimidin-4-ylamino)cyclohexanol (655 mg, 2.17 mmol), tri-o-tolylphosphine (298 mg, 0.979 mmol), ethyl acrylate (355 uL, 3.26 mmol) and palladium (II) acetate (73 mg, 0.33 mmol) in triethylamine (20 mL) was evacuated and back-filled with nitrogen (3×). The reaction mixture was heated overnight at 130° C., filtered and concentrated. The residue was purified by flash chromatography eluting with chloroform/7 N ammonia in methanol (0.5-5%) to afford the title compound (364 mg, 52%).

1. customwas evacuated
2. additionback-filled with nitrogen (3×)
3. filtrationfiltered
4. concentrationconcentrated
5. customThe residue was purified by flash chromatography
6. washeluting with chloroform/7 N ammonia in methanol (0.5-5%)