METHOD FOR THE PRODUCTION OF THE ALPHA FORM OF VORTIOXETINE HBr Russian patent published in 2022 - IPC C07D295/06 C07D295/96 

FIELD: chemistry.

SUBSTANCE: invention relates to a method for the production of crystalline vortioxetine HBr, characterized by reflections on an X-ray powder diffraction pattern (XRPD) at 5.85, 9.30, 17.49 and 18,58 (°2θ) (±0,1°), moreover, the method includes stages (a) of obtaining a solution of vortioxetine in practically pure toluene, and the purity of said practically pure toluene is above 90% (weight/weight), and the temperature of the solution obtained at stage a) is in the range from 0°C to the phlegm temperature, and the concentration of vortioxetine obtained at stage a) is from 10 g/l toluene to 500 g/l toluene; (b) mixing the specified solution obtained at stage a) with HBr and C₂-C₃ carboxylic acid at a temperature above 10°C up to 40°C or lower to obtain a mixture b); moreover, the molar ratio of HBr:C₂-C₃ carboxylic acid at stage b) is from 1:1 to 1:10 and (c) separation of the precipitate obtained at stage (b).

EFFECT: production of crystalline vortioxetine HBr, with a high yield.

10 cl, 14 ex, 17 dwg