反应详情

温度

40 °C

To a solution of 5-{[1-(N,N-dimethylglycyl)-5-(methyloxy)-2,3-dihydro-1H-indol-6-yl]amino}-8-fluoro-3-[(4-methylphenyl)sulfonyl]pyrrolo[2′,3′:4,5]pyrimido[6,1-b]quinazolin-7(3H)-one (265 mg, 0.404 mmol) in THF (5 mL) was added (1-methylethyl)amine (0.694 mL, 8.08 mmol). The resulting mixture was let stir at 40° C. for 16 h at which time it was diluted with ethyl acetate and washed with a saturated ammonium chloride solution, a saturated sodium bicarbonate solution, water and a saturated brine solution. Organics were dried over sodium sulfate and solvents removed under reduced pressure. Residue was purified via SiO2 chromatography to afford 2-({2-{[1-(N,N-dimethylglycyl)-5-(methyloxy)-2,3-dihydro-1H-indol-6-yl]amino}-7-[(4-methylphenyl)sulfonyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}amino)-6-fluoro-N-(1-methylethyl)benzamide. (210 mg, 0.294 mmol) as a yellow solid. (ESIMS (M+H)+=715)

1. washwashed with a saturated ammonium chloride solution
2. dry with materialOrganics were dried over sodium sulfate and solvents
3. customremoved under reduced pressure
4. customResidue was purified via SiO2 chromatography