反应详情

温度

90 °C

A mixture of 4-chloro-6-methoxy-7-(3-piperidinopropoxy)quinazoline (380 mg, 1.13 mmol), (prepared as described for the starting material in Example 67), potassium carbonate (469 mg, 3.4 mmol), 4-bromo-5-hydroxyindole (240 mg, 1.13 mmol) and DMA (4.0 ml) were stirred at 90° C. for 3 hours and allowed to cool to ambient temperature. The reaction mixture was filtered and the filtrate evaporated under vacuum. The residue was purified by column chromatography eluting with dichloromethane/methanolic ammonia (7M) (95/5) to give an oil. This oil was further purified by column chromatography eluting with dichloromethane/methanol (60/40) to give 4-(4-bromoindol-5-yloxy)-6-methoxy-7-(3-piperidinopropoxy)quinazoline (256 mg, 44%).

1. custom(prepared
2. temperatureto cool to ambient temperature
3. filtrationThe reaction mixture was filtered
4. customthe filtrate evaporated under vacuum
5. customThe residue was purified by column chromatography
6. washeluting with dichloromethane/methanolic ammonia (7M) (95/5)
7. customto give an oil
8. customThis oil was further purified by column chromatography
9. washeluting with dichloromethane/methanol (60/40)