| 主权项 |
1. A process for the manufacture of vortioxetine or pharmaceutically acceptable salts thereof, which process comprises reacting a compound of formula Iwherein each Hal independently represents fluoro or chloro; R′ represents H or R′ represents one or two moieties independently selected from CHO, COOH, COOR′″ or COONR′″2, or R′ represents one to five moieties independently selected from C1-6-alkyl; R′″ independently represents H or C1-6-alkyl; and X− represents a non-coordinating and non-nucleophilic anion, with an optionally protected piperazine of formula IIwherein R represents H or a protective group,and with a compound of formula IIIwherein R″ represents H or a cation, and an optional base in a solvent to obtain a compound of formula IVfollowed by a de-complexation step in which the optionally substituted cyclopentadienyliron is de-complexed, and an optional de-protection step in which the optionally protected piperazine moiety is de-protected to obtain 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine (vortioxetine). |
