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), (prepared as described for the starting material in Example 152), potassium carbonate (215 mg, 1.56 mmol) and 5-hydroxy-2-methylindole (162 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 was 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 6-methoxy-4-(2-methylindol-5-yloxy)-7-(3-(N-methyl-N-methylsulphonylamino)propoxy)quinazoline (166 mg, 35%).

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