Process for the preparation of 1-pyridyl-alkyl-4-aryl piperazines which are useful as antihypertensive compounds, their separation into the respective optical antipodes, and the stereoisomeric compounds so obtained
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United States of America Patent
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Mar 25, 1986
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N/A
app pub date -
Jul 3, 1984
filing date -
Jul 11, 1983
priority date (Note) -
Expired
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Abstract
A process for the preparation of 1-pyridyl-alkyl-4-aryl piperazines, in the racemic form, of the formula ##STR1## in which: the pyridine ring is alpha-, beta-, or gamma-substituted; R=H; C.sub.n H.sub.2n+1, n being in the range from 1 to 4; R'=H, halogen, CH.sub.3, OCH.sub.3, in which process: (a) pyridine aldehyde is reacted between -5.degree. C. and 0.degree. C. with (CH.sub.3).sub.2 S=CH.sub.2 ; (b) the oxirane so obtained is treated with an arylpiperazine; (c) the hydroxyl derivative obtained in (b), after salification with alkaline hydrides or hydrates in a solvent medium is treated with alkylating agents, and the separation of the compounds so obtained into the respective optical antipodes.
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