反应详情

Potassium carbonate (8.39 g) was dissolved in water (140 mL), followed by the addition of 7-(4-chlorobutoxy)-3,4-dihydrocarbostyril (19.4 g) and 1-(2,3-dichlorophenyl)piperazine monohydrochloride (16.2 g) thereto. The mixture was refluxed under stirring for about 3 hours. After reaction, the resulting mixture was cooled, and precipitated crystals were filtered. The crystals were dissolved in ethyl acetate (350 mL), and about 210 mL of water/ethyl acetate azeotrope was distilled under reflux. The remaining solution was cooled, and precipitated crystals were filtered. The thus-obtained crystals were dried at 60° C. for 14 hours, thereby obtaining 20.4 g of crude aripiprazole (yield: 74.2%).

1. temperatureThe mixture was refluxed
2. customAfter reaction
3. temperaturethe resulting mixture was cooled
4. customprecipitated crystals
5. filtrationwere filtered
6. dissolutionThe crystals were dissolved in ethyl acetate (350 mL)
7. distillationabout 210 mL of water/ethyl acetate azeotrope was distilled
8. temperatureunder reflux
9. temperatureThe remaining solution was cooled
10. customprecipitated crystals
11. filtrationwere filtered
12. customThe thus-obtained crystals were dried at 60° C. for 14 hours