反应详情

温度

85 °C

A suspension of 4-chloro-6-methoxy-7-(3-(4-methylsulphonylpiperazin-1-yl)propoxy)quinazoline (0.25 g, 0.66 mmol), 5-hydroxy-7-azaindole (0.089 g, 0.663 mmol), (prepared as described for the starting material in Example 2), and potassium carbonate (0.091 g, 0.66 mmol) in DMF (3 ml) was stirred at 85° C. for 3 hours. The mixture was filtered and the filtrate was purified by preparative LCtMS eluting with acetonitrile/water (containing 1% acetic acid). The fractions containing the expected product were combined and evaporated. The residue was dissolved in methylene chloride and washed with 0.5N aqueous ammonia followed by brine, dried (MgSO4) and evaporated. The residue was triturated under diethyl ether, filtered and dried under vacuum to give 4-(7-azaindol-5-yloxy)-6-methoxy-7-(3-(4-methylsulphonylpiperazin-1-yl)propoxy)quinazoline (0.138 g, 45%).

1. custom(prepared
2. filtrationThe mixture was filtered
3. customthe filtrate was purified by preparative LCtMS
4. washeluting with acetonitrile/water (containing 1% acetic acid)
5. additionThe fractions containing the expected product
6. customevaporated
7. dissolutionThe residue was dissolved in methylene chloride
8. washwashed with 0.5N aqueous ammonia
9. dry with materialdried (MgSO4)
10. customevaporated
11. customThe residue was triturated under diethyl ether
12. filtrationfiltered
13. customdried under vacuum