反应详情

To a stirred solution of N-(2-aminoethyl)-5-[4-(2-fluoro-5-{[(2-fluoro-5-methylphenyl)amino]carbonyl}phenoxy)pyridin-2-yl]-1H-pyrrole-3-carboxamide (80 mg, 0.16 mmol) in 10 ml of anhydrous DMF, were added N,N-diisopropylethylamine (60 mg, 0.47 mmol) and methyl bromoacetate (30 mg, 0.20 mmol). The mixture was stirred at room temperature for 1 hour and poured into 100 ml of water. The precipitates were filtered, washed with water, and dried in vacuo to give the crude, which was purified by silica gel chromatography eluting with a gradient of 3˜5% of methanol in chloroform to give methyl ({2-[({5-[4-(2-fluoro-5-{[(2-fluoro-5-methylphenyl)amino]carbonyl}phenoxy)pyridin-2-yl]-1H-pyrrol-3-yl}carbonyl)amino]ethyl}amino)acetate as white solid. Yield: 38 mg, 41%.

1. filtrationThe precipitates were filtered
2. washwashed with water
3. customdried in vacuo
4. customto give the crude, which
5. customwas purified by silica gel chromatography
6. washeluting with a gradient of 3˜5% of methanol in chloroform