VORTIOXETINE MANUFACTURING PROCESS Russian patent published in 2018 - IPC C07D295/96 C07F15/02 

FIELD: chemistry.

SUBSTANCE: invention relates to a process for the preparation of vortioxetine or a pharmaceutically acceptable salt thereof. Method comprises reacting a compound of formula I

wherein each Hal is independently fluoro or chloro; R' is H, or R' is one or two groups independently selected from CHO, COOH, COOR''' or COONR₂''', or R' represents one to five groups independently selected from C_1-6-alkyl; R''' is independently H or C_1-6-alkyl; and X^- is a non-coordinating and non-nucleophilic anion, with a piperazine of formula II

where R is H, and with a compound of formula III

where R'' is H or a cation, and a base, optionally in a solvent, to obtain a compound of formula IV

followed by a step of breaking down the complex to obtain 1- [2- (2,4-dimethylphenylsulfanyl) -phenyl] -piperazine (vortioxetine).

EFFECT: invention makes it possible to produce vortioxetine under non-stringent conditions, in high yield and using cheap starting materials.

12 cl, 1 dwg, 2 ex