PROCESS FOR THE PREPARATION OF PHARMACEUTICAL COMPOSITION BASED ON A piperazine derivative THAT IS ACTIVE IN RESPECT OF THE CENTRAL NERVOUS SYSTEM AND A painkilling LEND MEANS, METHOD OF PREPARATION OF THE piperazine AND THUS PREPARED PHARMACEUTICAL PREPARATION.

摘要

Phenylpiperazine derivatives having the general formula (I IMAGE in which R1 represents a radical S(O)mR3, S(O)nCF3 or IMAGE in which radicals m is 0, 1 or 2, n is 1 or 2, R3 is an alkyl radical having 1 to 10 carbon atoms and R4 and R5 independently represent a hydrogen atom or an alkyl radical having 1 to 4 carbon atoms, or the N atom, R4 and R5 together form a heterocyclic ring, which can contain another hetero- atom, and R2 represents a hydrogen atom, the radical CH2-CH2-OH or a radical of formula CH2-CH2-O-COR6, CH2-CH2-O-CONHR6 or CH@CH2-O-R6, in which radicals R6 being an alkyl radical having 1 to 6 carbon atoms and their pharmaceutically acceptable acid addition salts are useful psychotropic agents and analgesics. Compounds in which R1 is -SCH3 and simultaneously R2 is H are not part of the invention. These derivatives can be prepared by reacting an aniline derivative of formula IMAGE with a compound of formula IMAGE in which X represents a halogen atom or OH, alkyl-SO3 or aryl-SO3 group or the two X symbols together represent a divalent oxygen atom, thereby completing a morpholine ring.