反应详情

温度

60 °C

A mixture of 7-hydroxy-6-methoxy-4-(3-methylindol-5-yloxy)quinazoline (1.35 g, 4.2 mmol), (prepared as described for the starting material in Example 271), potassium carbonate (1.74 g, 12.6 mmol) and (2R)-(−)-glycidyl tosylate (1.92 g, 8.4 mmol) in DMF (25 ml) was stirred at 60° C. for 2 hours and allowed to cool to ambient temperature. The reaction mixture was filtered and the solvent removed in vacuo. The residue was dissolved in dichloromethane and washed with saturated sodium hydrogen carbonate solution. The organic layer was then dried (MgSO4), filtered and solvent removed in vacuo to give a solid. This was triturated with ether and the solid filtered off and dried to give (2R)-6-methoxy-4-(3-methylindol-5-yloxy)-7-(oxiran-2-ylmethoxy)quinazoline (842 mg, 53%).

1. custom(prepared
2. temperatureto cool to ambient temperature
3. filtrationThe reaction mixture was filtered
4. customthe solvent removed in vacuo
5. dissolutionThe residue was dissolved in dichloromethane
6. washwashed with saturated sodium hydrogen carbonate solution
7. dry with materialThe organic layer was then dried (MgSO4)
8. filtrationfiltered
9. customsolvent removed in vacuo
10. customto give a solid
11. customThis was triturated with ether
12. filtrationthe solid filtered off
13. customdried