反应详情

温度

90 °C

To a solution of methyl 3-(6-fluoro-3,4-dihydroquinolin-1(2H)-yl)-2-(trifluoromethylsulfonyloxy)quinoxaline-6-carboxylate (From Ex. 6, step 3, 200 mg, crude) in dioxane (5.0 mL) and three drops of water was added 5-fluorobenzofuran-2-ylboronic acid (210 mg, 1.07 mmol), K3PO4 (272 mg, 1.29 mmol) and Pd(PPh3)4 (25 mg, 0.02 mmol). The reaction was stirred for 1 h at 90° C. under an inert atmosphere of nitrogen in an oil bath. The reaction mixture was concentrated under vacuum to give the residue, which was purified by a silica gel column with 1% to 5% ethyl acetate in petroleum to afford methyl 2-(5-fluoro-1H-inden-2-yl)-3-(6-fluoro-3,4-dihydroquinolin-1(2H)-yl)quinoxaline-6-carboxylate as a light red solid (59 mg).

1. concentrationThe reaction mixture was concentrated under vacuum
2. customto give the residue, which
3. customwas purified by a silica gel column with 1% to 5% ethyl acetate in petroleum