反应详情

温度

100 °C

A mixture of 4-chloro-6-methoxy-7-(3-(N-methyl-N-methylsulphonylamino)propoxy)quinazoline (360 mg, 1.00 mmol), potassium carbonate (215 mg, 1.56 mmol) and 5-hydroxyindole (147 mg, 1.10 mmol) in DMF (8.0 ml) was stirred at 100° C. for 5 hours and allowed to cool to ambient temperature. The solvent was removed by evaporation and the residue purified by silica column chromatography eluting with methanol (2.5 to 5%) in dichloromethane. The resulting solid was recrystallised from ethyl acetate, filtered and washed with diethyl ether to give 4-(indol-5-yloxy)-6-methoxy-7-(3-(N-methyl-N-methylsulphonylamino)propoxy)quinazoline (77 mg, 17%).

1. temperatureto cool to ambient temperature
2. customThe solvent was removed by evaporation
3. customthe residue purified by silica column chromatography
4. washeluting with methanol (2.5 to 5%) in dichloromethane
5. customThe resulting solid was recrystallised from ethyl acetate
6. filtrationfiltered
7. washwashed with diethyl ether