反应详情

50 mg 5-{6-[3-(4-fluorophenyl)-1-trityl-1H-pyrazol-4-yl]quinazolin-4-yl}thiophen-2-sulfonic acid methylamide (compound in Example 745) was dissolved in 3 mL N,N-dimethylformamide, then 3.1 mg sodium hydride was added thereto and stirred at room temperature for 0.5 hour. Under ice-cooling, a solution of 18 mg 4-methoxyphenacyl bromide in 2 mL N,N-dimethylformamide was added thereto and stirred for 1.0 hour under ice-cooling. Water was added to the reaction solution which was then extracted with ethyl acetate, and the organic layer was washed with brine and dried over sodium sulfate. The solvent was evaporated, and the residue was purified by silica gel column chromatography (ethyl acetate/hexane) to give 47 mg of the title compound.

1. temperatureUnder ice-cooling
2. stirringstirred for 1.0 hour under ice-
3. temperaturecooling
4. extractionwas then extracted with ethyl acetate
5. washthe organic layer was washed with brine
6. dry with materialdried over sodium sulfate
7. customThe solvent was evaporated
8. customthe residue was purified by silica gel column chromatography (ethyl acetate/hexane)