反应详情

A mixture of aripiprazole (1.5 g, 3.3 mmol), dibenzylcarbamoyl chloride (1.74 g, 6.7 mmol) silver carbonate (3.75 g, 13.4 mmol) and 2-methyltetrahydrofuran (30 mL) was heated at reflux for 4 days. The reaction mixture was cooled, diluted with ethyl acetate and water, and then filtered through celite. The organic phase was separated, dried over MgSO4 and evaporated. The residue obtained was further purified on silica eluting with ethyl acetate/tetrahydrofuran to give after evaporation of the major product containing fractions, Compound-80 (1.02 g) was a yellow oil.

1. temperaturewas heated
2. temperatureat reflux for 4 days
3. temperatureThe reaction mixture was cooled
4. filtrationfiltered through celite
5. customThe organic phase was separated
6. dry with materialdried over MgSO4
7. customevaporated
8. customThe residue obtained
9. customwas further purified on silica eluting with ethyl acetate/tetrahydrofuran
10. customto give
11. customafter evaporation of the major product
12. additioncontaining fractions, Compound-80 (1.02 g)