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 5 mL tetrahydrofuran, then 0.07 mL of 1.0 M lithium bistrimethyl silyl amide was added thereto under ice-cooling, and the mixture was stirred for 0.5 hour. Under ice-cooling, a solution of 80 mg 3-methoxyphenacyl bromide in 2 mL tetrahydrofuran was added thereto and stirred for 1.5 hour. 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 17 mg of the title compound.

1. temperatureunder ice-cooling
2. temperatureUnder ice-cooling
3. stirringstirred for 1.5 hour
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)