反应详情

To a stirred solution of 4-(3-bromo-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-pyrrolo[2,3-b]pyridin-4-yloxy)-3-fluorobenzenamine (400 mg, 0.85 mmol), 2-fluoro-6-methoxybenzoic acid (226 mg, 1.33 mmol), and HATU (641 mg, 1.33 mmol) in DMF (6 mL) was added DIPEA (387 mg, 3 mmol), followed by DMAP (50 mg). The resulting mixture was stirred at rt overnight, diluted with EtOAc, and washed with saturated aq. K2HPO4 solution and brine. The organic layer was dried over MgSO4 and concentrated in vacuo. The residue was purified by flash column chromatography (silica gel, eluting with 30% EtOAc/CH2Cl2) to give the desired product (370 mg, 72%) as a white solid. LC/MS(ESI+) m/z 605 (M+H)+.

1. washwashed with saturated aq. K2HPO4 solution and brine
2. dry with materialThe organic layer was dried over MgSO4
3. concentrationconcentrated in vacuo
4. customThe residue was purified by flash column chromatography (silica gel, eluting with 30% EtOAc/CH2Cl2)