Neuroleptic 1-aralkyl-4-phenyl-piperazines prodn - by reacting ethylenediamines with oxalic acid derivs,and reducing resulting dioxo

摘要

Title 1-aralkyl-4-phenyl-piperazines of formula (I): (where Ar is an aromatic residue with 2 fused rings of which the one not linked to the rest of the molecule may be an iso- or heterocyclic satd. or aromatic ring, and R1 and R2 are H, halogen, amino, acylamino, CN, CF3 or 1-4C alkyl, alkoxy, alkylcarbonyl or alkylthio) are prepd. by reacting an ethylene-diamine deriv. of formula (II): with a cpd. X-CO-CO-X (where X is halogen or lower alkoxy) and reducing the resulting dioxo-piperazine cpd. (III): with metal hydrides (e.g. LiAlH4, sodium bis-(2-methoxyethoxy)-aluminium hydride or diborane). (I) thus obtained may be converted into a physiologically tolerable acid addn. salt. The process uses very readily available starting materials and proceeds smoothy and with good yields; sterically hindered products are easily produced.