反应详情

1,4-Dioxane (12 mL) and N,N′-dimethylethylenediamine (86 μL) were added to a mixture of (4-bromo-2-fluorophenyl)[4-(5-cyclopropyl-3-methylpyridin-2-yl)piperazin-1-yl]methanone (325 mg) described in Preparation Example 121, 3-benzyloxymethyl-5-methylimidazolidine-2,4-dione (225 mg) described in Preparation Example 206, cesium carbonate (521 mg) and copper(I) iodide (76 mg), and the mixture was stirred with heating under reflux for 10 hr. The reaction mixture was cooled, water was added, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine, dried over sodium sulfate, and the solvent was evaporated. The obtained residue was purified by column chromatography (hexane:ethyl acetate) to give the title is compound (270 mg).

1. temperaturewith heating
2. temperatureunder reflux for 10 hr
3. temperatureThe reaction mixture was cooled
4. extractionthe mixture was extracted with ethyl acetate
5. washThe organic layer was washed with saturated brine
6. dry with materialdried over sodium sulfate
7. customthe solvent was evaporated
8. customThe obtained residue was purified by column chromatography (hexane:ethyl acetate)
9. customto give the title