The preparation of new 4-aryl-hexahydropyridol 1,2-c]pyrimidine derivatives III-XXVI with an arylpiperazinylbutyl moiety in N-2 position has been described. Multi-stage synthesis techniques were used to obtain 4-arylhexahydro-1H,3H-pyrido[1,2-c]pyrimidine-1,3-dione Ia-f derivatives, being the starting compounds for further modification. N-alkylation of the imide group in compounds Ia-f followed, using 1,4-dibromobutane to yield bromobutyl derivatives IIa-f. The final products III-XXVI were obtained by condensation of aryl- or heteroaryl- piperazine with the bromobutyl derivatives IIa-f. Compounds XII, XIV, XIX, XX, XXIV-XXVI will be submitted to a pharmacological investigation for their affinity towards 5-HT1A, 5-HT2A and alpha1 adrenergic receptor, using radioligand binding assay.