反应详情

温度

100 °C

A mixture of 4-chloro-6-methoxy-7-(3-piperidinopropoxy)quinazoline (84 mg, 0.24 mmol), (prepared as described for the starting material in Example 67), potassium carbonate (162 mg, 1.18 mmol) and ethyl 7-chloro-5-hydroxyindole-2-carboxylate (62 mg, 0.26 mmol) in DMA (2.0 ml) was stirred at 100° C. for 2 hours and allowed to cool to ambient temperature. The reaction mixture was filtered and the filtrate evaporated. The residue was purified by silica column chromatography using gradient elution dichloromethane with 2.5%, 5%, 10% methanol, then dichloromethane with 2% ammonia) to give 4-(7-chloro-2-(ethoxycarbonyl)indol-5-yloxy)-6-methoxy-7-(3-piperidinopropoxy)quinazoline (78 mg, 63%).

1. custom(prepared
2. temperatureto cool to ambient temperature
3. filtrationThe reaction mixture was filtered
4. customthe filtrate evaporated
5. customThe residue was purified by silica column chromatography
6. washelution dichloromethane with 2.5%, 5%, 10% methanol