Process for preparing 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine or pharmaceutically acceptable salt thereof
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Abstract
This disclosure relates to a process for the preparation of 1-[2-(2,4-dimethylphenylsulfanyl) -phenyl]piperazine or a pharmaceutically acceptable salt thereof. The process includes reacting compound II with compound III and compound IV
in the presence of a solvent, a base and a palladium catalyst. R, R′, Xi, and X2 in the formulas above are defined in the Specification.
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28 Claims
- 1. A process for the preparation of
- 25. A process for the manufacturing of 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine hydrobromic acid addition salt in which process 1-1.5 equivalents of 2,4-dimethylthiolphenol, piperazine, and one of 1-bromo-2-iodo -benzene and 1,2-dibromo-benzene are dispersed in toluene followed by the addition of 2-5 equivalents NaO(t-Bu) and 1-2 mole-% Pd2dba3 and rac-BINAP dispersed in toluene to obtain a mixture which is heated to reflux 3-5 hours to obtain the product 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine, which is further reacted with aqueous hydrobromic acid.
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26. A process for the manufacturing of 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine hydrobromic acid addition salt in which process 2-5 equivalents of NaO (t-Bu), 2-5 equivalents piperazine, 0.2-0.6 mole-% Pddba2, and 0.6-1 mole-% rac-BINAP are dispersed in toluene to obtain mixture A′
- , to which mixture approximately 1 equivalent 2-bromo-iodobenzene is added to obtain mixture B′
, to which mixture 1 equivalent 2,4-dimethylthiophenol is added and the resulting mixture is heated to reflux for 4-6 hours to obtain 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine, which is further reacted with aqueous hydrobromic acid. - View Dependent Claims (28)
- , to which mixture approximately 1 equivalent 2-bromo-iodobenzene is added to obtain mixture B′
Specification