反应详情

温度

120 °C

(4-[1-[(5-Chloro-2,4-dimethoxy-phenylcarbamoyl)-methyl]-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl}-phenyl)-acetic acid ethyl ester (Intermediate K) (105.4 mg, 0.19 mmol) is added to a stirred solution of Bis(tributyltin)oxide) (2 eq, 0.38 mmol, 193.1 μL) in toluene (10 ml). The mixture is heated at reflux at 120° C. for 72 hours. The toluene is removed in vacuo, and the red/brown oily residue is partitioned between EtOAc and saturated NaHCO3 (5 ml). The resultant precipitate is filtered, washed with NaHCO3, EtOAc, 1M HCl, water, and dried to give the title compound, [M+H]+ 524

1. temperatureThe mixture is heated
2. customThe toluene is removed in vacuo
3. customthe red/brown oily residue is partitioned between EtOAc and saturated NaHCO3 (5 ml)
4. filtrationThe resultant precipitate is filtered
5. washwashed with NaHCO3, EtOAc, 1M HCl, water
6. customdried