反应详情

温度

100 °C

To a degassed solution of N-methyl-6-(N-methylmethylsulfonamido)-2-(2-methylthiazol-5-yl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzofuran-3-carboxamide (200 mg, 0.40 mmol), 2-chloro-11-fluoro-5,6-dihydroindolo[1,2-h][1,7]naphthyridine (113 mg, 0.41 mmol), Na2CO3 (84 mg, 0.79 mmol), K2CO3 (109 mg, 0.79 mmol) in 1,4-dioxane (5 mL) and H2O (0.1 mL) were added Pd2(dba)3 (10 mg) and X-Phos (10 mg) under N2. Then the mixture was stirred at 100° C. for 2 hours. The reaction mixture was cooled to RT and filtered. The filtrate was washed with H2O and dried over Na2SO4. After concentrated, the residue was purified by prep-HPLC to give the product (30 mg, yield: 12%). 1H-NMR (CDCl3, 400 MHz) δ 8.41 (s, 1H), 7.89 (s, 1H), 7.62˜7.68 (m, 2H), 7.45 (d, J=7.6 Hz, 1H), 7.24 (s, 1H), 7.12˜7.20 (m, 2H), 6.74˜6.81 (m, 1H), 6.22 (d, J=4.0 Hz, 1H), 4.32 (t, J=6.4 Hz, 2H), 3.32 (s, 3H), 3.27˜3.31 (m, 2H), 3.02 (d, J=4.8 Hz, 3H), 2.75 (s, 3H), 2.74 (s, 3H). MS (M+H)+: 616.

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