Process for the Manufacture of 1-[2-(2,4-Dimethyl-Phenylsulfanyl)-Phenyl]-Piperazine

摘要

A process for the manufacture of 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine and pharmaceutically acceptable salts is disclosed that involves reacting compounds of formula II, III, IV under Pd catalysis and in presence of phosphine ligands to give Compound I.;

主权项

1. A process for the manufacture of or pharmaceutically acceptable salts thereof (Compound I), said method comprising reacting a compound of formula II wherein X represents Br or I, with a compound of formula III wherein Y represents Cl or Br and R′ represents hydrogen or a metal ion, and a compound of formula IV wherein R represents hydrogen or a protective group, in the presence of a solvent, a base and a palladium catalyst consisting of a palladium source and a phosphine ligand at a temperature between 50° C. and 130° C.