Réaction #316744

Équation de réaction

bupropion

HBr

→

bupropion hydrobromide

Rendement 74.8%

Solvants

isopropanol

Conditions de réaction

Traitement

1. 1
   AutreA 250 ml flask equipped with overhead stirrer and gas inlet
2. 2
   TempératureThe solution was maintained
3. 3
   workup.ADDITIONDuring the gas addition a heavy white precipitate
4. 4
   Autreformed
5. 5
   workup.ADDITIONAt the end of the gas addition the temperature of the mixture
6. 6
   Températurewas raised
7. 7
   Températureto reflux (80° C.)
8. 8
   Autreto get complete solution of the suspended solid
9. 9
   Autrefurther lowered to 0-5° C. in 1 additional hour
10. 10
    AutreThe precipitate obtained
11. 11
    Filtrationwas filtered
12. 12
    Lavagewashed with 20 ml of cold isopropanol
13. 13
    AutreThe discharged wet solid was dried under vacuum (30 mmHg) in a static drier at 50° C. for 16 hours

Mode opératoire

A 250 ml flask equipped with overhead stirrer and gas inlet was charged with 34 g of bupropion base and 138 ml of isopropanol. The solution was maintained under stirring while 13 g of gaseous HBr was introduced through the gas inlet in a time of 20′ while the internal temperature of the mixture raises from 25 to 40° C. During the gas addition a heavy white precipitate formed. At the end of the gas addition the temperature of the mixture was raised to reflux (80° C.), to get complete solution of the suspended solid. The temperature was then lowered to 25° C. in 1 hour and further lowered to 0-5° C. in 1 additional hour. The precipitate obtained was filtered and washed with 20 ml of cold isopropanol. The discharged wet solid was dried under vacuum (30 mmHg) in a static drier at 50° C. for 16 hours. 34 g of bupropion hydrobromide form I were obtained.

Source