反应详情

To a mixture of [4-(3,5-dicyclopropylpyridin-2-yl)piperazin-1-yl](4-iodophenyl)methanone (473 mg) described in Preparation Example 95, (R)-4-ethyloxazolidin-2-one (138 mg) described in Preparation Example 26, potassium carbonate (415 mg) and copper (I) iodide (38 mg) were added toluene (2 mL) and N,N′-dimethylethylenediamine (43 μL), and the mixture was heated under reflux for 3 hr. The reaction mixture was cooled, ethyl acetate and aqueous ammonium chloride solution were added and the mixture was extracted with ethyl acetate. The ethyl acetate layer was washed with a 1:1 mixture of saturated aqueous ammonium chloride solution and ammonium water, washed once with saturated aqueous ammonium chloride solution, once with saturated aqueous sodium chloride solution, and dried over sodium sulfate. The solvent was evaporated under reduced pressure. The residue was purified by column chromatography (chloroform:methanol) to give the title compound (377 mg).

1. temperaturethe mixture was heated
2. temperatureunder reflux for 3 hr
3. temperatureThe reaction mixture was cooled
4. extractionthe mixture was extracted with ethyl acetate
5. washThe ethyl acetate layer was washed with a 1:1 mixture of saturated aqueous ammonium chloride solution and ammonium water
6. washwashed once with saturated aqueous ammonium chloride solution, once with saturated aqueous sodium chloride solution
7. dry with materialdried over sodium sulfate
8. customThe solvent was evaporated under reduced pressure
9. customThe residue was purified by column chromatography (chloroform:methanol)