PROCESS FOR THE PREPARATION OF VORTIOXETINE SALTS

摘要

The invention relates to an improved process for the preparation of pharmaceutical active ingredients and also to high purity salts and pharmaceutical compositions prepared by said process. More particularly the invention relates to an economical process for the preparation of the compound having the international non-proprietary name (INN) vortioxetine and the chemical nomenclature 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine. Vortioxetine corresponds to the following Formula;;Still more particularly the invention relates to the preparation of high purity vortioxetine L-(+)-mandelate salt of the Formula IX, the conversion of this salt into other highly pure salts and also to the formulation of said salts.

主权项

1. Process for the preparation of vortioxetine salts of the general Formula VII by reacting the compound of the Formula V with a compound of the general Formula VI (wherein X stands for chlorine, bromine, iodine, methanesulfonyloxy, p-toluenesulfonyloxy or hydroxy; HnA represents an organic or inorganic mono- or polybasic acid, A is an acid residue and n is the number of the hydrogen atoms, preferably 1, 2 or 3 which comprises converting the vortioxetine base of the Formula I formed in the L-(+)-mandelic acid salt of the Formula IX, if necessary setting free the base from the salt and converting the same in another salt of the general Formula VII (wherein HnA stands for a mono- or polybasic organic or inorganic acid; n is 1, 2 or 3 and A represents an acid residue ion).