反应详情

A mixture of trimethylboroxine (27 μL, 0.19 mmol), Pd(dppf)2Cl2 (22 mg, 0.019 mmol), Cs2CO3 (185 mg, 0.57 mmol) and N-(2-chloro-pyrimidin-5-yl)-3,4-difluoro-benzamide (H) (50 mg, 0.19 numol) in dioxane (1 mL)/H2O (0.1 mL) was heated at 110–130° C. (bath temperature) for 1 h. The crude reaction mixture was filtered through a pad of celite and concentrated under reduced pressure. Purification of the crude material by column chromatography (hexanes/EtOAc) gave the desired product as white solid (27 mg, 57%).

1. temperaturewas heated at 110–130° C. (bath temperature) for 1 h
2. customThe crude reaction mixture
3. filtrationwas filtered through a pad of celite
4. concentrationconcentrated under reduced pressure
5. customPurification of the crude material by column chromatography (hexanes/EtOAc)