反应详情

To a mixture of (4-bromo-2-methylphenyl)[4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl]methanone (842 mg) described in Preparation Example 118, sodium iodide (650 mg) and copper(I) iodide (246 mg) were added toluene (2.2 mL) and N,N′-dimethylethylenediamine (1.62 mL), and the mixture was stirred with heating under reflux for 18 hr under a nitrogen stream. The reaction mixture was cooled, water was added, and the mixture was extracted with ethyl acetate. The solvent was evaporated from the organic layer, and the residue was purified by column chromatography (chloroform:methanol) to give the title compound (562 mg).

1. temperaturewith heating
2. temperatureunder reflux for 18 hr under a nitrogen stream
3. temperatureThe reaction mixture was cooled
4. extractionthe mixture was extracted with ethyl acetate
5. customThe solvent was evaporated from the organic layer
6. customthe residue was purified by column chromatography (chloroform:methanol)