Vortioxetine hydrobromide → Vortioxetine

Participants

Reaction Conditions

Reaction Steps

1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine-HBr (33.1 Kg) in a mixture of isopropanol (412 L) and water (18 L) was heated to reflux. The solution was cooled to 20° C. and isopropanol solvate of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine was isolated by filtration and washed with isopropanol (82 L). The wet filter cake was dissolved in a mixture of isopropanol (353 L) and water (17 L) at reflux. The solution was cooled to 20° C. and isopropanol solvate of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine was isolated by filtration and washed with isopropanol (74 L). The wet filter cake was dissolved in a mixture of toluene (132 L) and water (13 L) at 80° C. and blank filtered. Water and isopropanol were distilled out of the reactor (55 L), distillation was stopped when distillate reached 102° C. Water (7 L) was then added and the solution was cooled to 20° C. slowly. 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine-HBr was isolated by filtration, filter cake washed with toluene (77 L) and dried. The amounts of impurities were less than 0.05% of compound 1, less than 0.015% of compound 2 and less than 0.05% of compound 3.

Provenance & Evidence