Process for the preparation of 1-pyridylalkyl-4-arylpiperazines, their separation into the respective optical antipodes (enantiomorphs) and the stereoisomers thus obtained

摘要

Process for the preparation of 1-pyridylalkyl-4-arylpiperazines, which, in their racemic form, have the general formula: in which: the pyridine ring is substituted at the alpha, beta or gamma position; the R symbol represents hydrogen or a CnH2n+1 group, n being a number from 1 to 4; and R' represents a hydrogen or halogen atom or a CH3 or OCH3 group; which process is characterised in that: a. the pyridinealdehyde is reacted between -5 DEG C and 0 DEG C with (CH3)2S=CH2; b. the oxirane thus formed is treated with an arylpiperazine; and c. the hydroxylated derivative obtained in Stage b. is treated, after salification with an alkali metal hydride or hydroxide in a solvent medium, with an alkylating agent; and separation of the compounds thus obtained into their enantiomorphs.