反应详情

温度

140 °C

To a solution of 1-nitro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-dibenzofuran (12, 0.30 mmol, 0.10 g) in anhydrous dioxane (2 ml) was added trifluoro-methanesulfonic acid 2-morpholin-4-yl-4-oxo-4H-1-benzopyran-8-yl ester (0.24 mmol, 0.091 g, see WO 03/024949), potassium carbonate (0.6 mmol, 0.083 g) and tetrakis (triphenylphosphine) palladium (0.015 mmol, 0.018 g). The reaction vessel was sealed and heated under the influence of microwave radiation (140° C., 10 minutes, low absorption setting). Upon completion the reaction mixture was filtered through a thin pad of silica and the cake washed with CH2Cl2. The solvents were then removed in vacuo to give a light brown solid residue (0.13 g, 100%) which was used without further purification. m/z 443.4 [M+H]+ (Rt=4.76 min).

1. customThe reaction vessel was sealed
2. filtrationUpon completion the reaction mixture was filtered through a thin pad of silica
3. washthe cake washed with CH2Cl2
4. customThe solvents were then removed in vacuo