反应详情

温度

100 °C

A mixture of 105d (2.06 g, 10 mmol), 3,5-dibromo-1-methylpyridin-2(1H)-one (2.65 g, 10 mmol), Pd2(dba)3 (91.6 mg, 0.1 mmol) Xant-phos (116 mg, 0.2 mmol), Cs2CO3(9.78 g, 30 mmol) in dioxane (100 mL) was degassed and stirred at 100° C. for 16 h under nitrogen. The reaction mixture was concentrated and the residue was purified by silica gel chromatography (EA/PE=5/1) to give N-(2-(6-(5-bromo-1-methyl-2-oxo-1,2-dihydropyridin-3-ylamino)pyridin-2-ylamino)ethyl)acrylamide 105e (2.54 g, 65%) as yellow solid. MS-ESI: [M+H]+ 394.1.

1. customwas degassed
2. concentrationThe reaction mixture was concentrated
3. customthe residue was purified by silica gel chromatography (EA/PE=5/1)