Reacción #1605835

Ecuación de reacción

aripiprazole

dibenzylcarbamoyl chloride

2-methyltetrahydrofuran

→

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

Disolventes

ethyl acetate

water

Condiciones de reacción

Tratamiento posterior

1. 1
   Temperaturawas heated
2. 2
   Temperaturaat reflux for 4 days
3. 3
   TemperaturaThe reaction mixture was cooled
4. 4
   Filtraciónfiltered through celite
5. 5
   OtroThe organic phase was separated
6. 6
   Secadodried over MgSO4
7. 7
   Otroevaporated
8. 8
   OtroThe residue obtained
9. 9
   Otrowas further purified on silica eluting with ethyl acetate/tetrahydrofuran
10. 10
    Otroto give
11. 11
    Otroafter evaporation of the major product
12. 12
    workup.ADDITIONcontaining fractions, Compound-80 (1.02 g)

Procedimiento

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.

Fuente