Реакция #1605835

Уравнение реакции

aripiprazole

dibenzylcarbamoyl chloride

2-methyltetrahydrofuran

→

7-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butoxy)-3,4-dihydroquinolin-2-yl dibenzylcarbamate

Растворители

ethyl acetate

water

Условия реакции

Обработка

1. 1
   Температураwas heated
2. 2
   Температураat reflux for 4 days
3. 3
   ТемператураThe reaction mixture was cooled
4. 4
   Фильтрацияfiltered through celite
5. 5
   ДругоеThe organic phase was separated
6. 6
   Сушкаdried over MgSO4
7. 7
   Другоеevaporated
8. 8
   ДругоеThe residue obtained
9. 9
   Другоеwas further purified on silica eluting with ethyl acetate/tetrahydrofuran
10. 10
    Другоеto give
11. 11
    Другоеafter evaporation of the major product
12. 12
    workup.ADDITIONcontaining fractions, Compound-80 (1.02 g)

Методика

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.

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