PIPERAZINE DERIVATIVES, THEIR SALTS AND METHOD OF THEIR PREPARATION

Pharmaceutically active piperazine derivatives, particularly piperazines substituted in position 1 with a 2-(2-chloro-10,11-dihydrodibenzo(b,f)thiepin-10-yloxy)ethyl residue and in position 4 a hydrogen atom or a methyl, 2-hydroxyethyl, 3-hydroxypropyl, 2-(aminocarbonyl)ethyl, 2-(acetoxy)ethyl or 2...

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Hauptverfasser: POMYKACEK JOSEF,CS, VALCHAR MARTIN RNCSC.,CS, PROTIVA MIROSLAV DRSC.,CS, DLOHOZKOVA NATASA RNCSC.,CS, JILEK JIRI RNDRSC.,CS
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Sprache:eng
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Zusammenfassung:Pharmaceutically active piperazine derivatives, particularly piperazines substituted in position 1 with a 2-(2-chloro-10,11-dihydrodibenzo(b,f)thiepin-10-yloxy)ethyl residue and in position 4 a hydrogen atom or a methyl, 2-hydroxyethyl, 3-hydroxypropyl, 2-(aminocarbonyl)ethyl, 2-(acetoxy)ethyl or 2 (decanoyloxy)ethyl group, their acid addition salts and processes for the preparation thereof. The compounds are noncataleptic neuroleptics with high affinity to dopamine D-2 receptors and with in vivo antidopaminergic activity but only slight sedative, adrenolytic and anticholinergic properties; but use as antipsychotic drugs free of undesirable side effects. Said compounds are available by several routes, such as (a) reaction of 10-(2-bromo-ethoxy)-2-chloro-10,11-dihydrodibenzo(b,f)thiepin with piperazine, 1-methylpiperazine, 2-(1-piperazinyl)ethanol, or 3-(1 piperazinyl)propanol and (b) acylation of aminoalcohols obtained by the preceding method with chlorides of the corresponding aliphatic carboxylic acids. Preferred addition salts are succinates, maleates, hydrochlorides and methanesulphonates prepared by the respective neutralization reactions.