反应详情

温度

95 °C

A mixture of 4-chloro-6-methoxy-7-(3-piperidinopropoxy)quinazoline (200 mg, 0.6 mmol), (prepared as described for the starting material in Example 67), potassium carbonate (248 mg, 1.8 mmol) and 5-hydroxy-6-methoxyindole (127 mg, 0.78 mmol) in DMA (4.0 ml) was stirred at 95° C. for 2.5 hours. The reaction mixture was allowed to cool to ambient temperature, filtered and the filtrate evaporated under vacuum. The residue was purified by silica column chromatography eluting with dichloromethane/methanol/0.880 aqueous ammonia (89/10/1) and the resulting oil triturated with diethyl ether to give 4-(6-methoxyindol-5-yloxy)-6-methoxy-7-(3-piperidinopropoxy)quinazoline (106 mg, 38%).

1. custom(prepared
2. temperatureto cool to ambient temperature
3. filtrationfiltered
4. customthe filtrate evaporated under vacuum
5. customThe residue was purified by silica column chromatography
6. washeluting with dichloromethane/methanol/0.880 aqueous ammonia (89/10/1)
7. customthe resulting oil triturated with diethyl ether