反应详情

A solution of PdCl2(dppf)-CH2Cl2 adduct (0.159 g, 0.194 mmol), (2-methoxy-4-(trifluoromethyl)phenyl)boronic acid (0.940 g, 4.27 mmol), 7-bromo-4-chloro-2-methylquinazoline (ACES Pharma, 1.000 g, 3.88 mmol), and potassium carbonate (2.147 g, 15.53 mmol) in 12 mL dioxane was treated with 4 mL water and was allowed to stir overnight at room temperature. LC/MS showed mostly product, so the aqueous layer was removed, and the reaction mixture was concentrated. Purification of the crude residue by silica gel column chromatography (0-50% EtOAc/heptane) gave 7-bromo-4-(2-methoxy-4-(trifluoromethyl)phenyl)-2-methylquinazoline (0.797 g, 2.007 mmol, 51.7% yield). (M+H)+=396.9.

1. customso the aqueous layer was removed
2. concentrationthe reaction mixture was concentrated
3. customPurification of the crude residue by silica gel column chromatography (0-50% EtOAc/heptane)