反应详情

温度

100 °C

To a degassed solution of 2-chloro-10-fluoro-5,6-dihydroindolo[1,2-h][1,7]naphthyridine (50 mg, 0.18 mmol) and 2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonamido)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzofuran-3-carboxamide (80 mg, 0.16 mmol) in 1,4-dioxane (5 mL), Pd2(dba)3 (10 mg), X-Phos (10 mg) and K3PO4 (100 mg, 0.38 mmol) were added under N2. After heated to 100° C. for 1 hour, the reaction mixture was cooled to RT, filtered and washed with EtOAc. The filtrate was washed with H2O, brine, dried over Na2SO4. After concentrated, the residue was purified by prep-HPLC to give the product (60 mg, yield: 61.5%). 1H-NMR (CDCl3, 400 MHz) δ 7.99 (s, 1H), 7.92˜7.98 (m, 2H), 7.65˜7.67 (m, 2H), 7.43 (d, J=7.6 Hz, 1H), 7.28˜7.32 (m, 2H), 7.15˜7.24 (m, 3H), 6.98˜7.03 (m, 1H), 6.05 (br s, 1H), 4.31 (t, J=6.4 Hz, 2H), 3.36 (s, 3H), 3.30 (t, J=6.4 Hz, 2H), 2.97 (d, J=4.8 Hz, 3H), 2.68 (s, 3H). MS (M+H)+: 613.

1. temperaturethe reaction mixture was cooled to RT
2. filtrationfiltered
3. washwashed with EtOAc
4. washThe filtrate was washed with H2O, brine
5. dry with materialdried over Na2SO4
6. concentrationAfter concentrated
7. customthe residue was purified by prep-HPLC