反应详情

Diisopropylethylamine (72 μl, 0.41 mmol) and methanesulphonyl chloride (32 μl, 0.41 mmol) were added to a suspension of 4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-(piperidin-4-ylmethoxy)quinazoline (150 mg, 0.34 mmol), (prepared as described for the starting material in Example 11), in methylene chloride (4 ml). After a few minutes all the material had gone into solution. The mixture was stirred for 3 hours at ambient temperature, washed with saturated sodium hydrogen carbonate solution, dried (MgSO4) and concentrated under reduced pressure. The solid was suspended in methanol and filtered to give 4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-{[1-(methylsulfonyl)piperidin-4-yl]methoxy}quinazoline (83 mg, 47%).

1. custom(prepared
2. waitAfter a few minutes all the material had gone into solution
3. washwashed with saturated sodium hydrogen carbonate solution
4. dry with materialdried (MgSO4)
5. concentrationconcentrated under reduced pressure
6. filtrationfiltered