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Herold F, Krol M, Kleps J: Synthesis of new hexahydro- and octahydropyrido [1,2-c] pyrimidine derivatives with an arylpiperazine moiety as ligands for 5-HT1A and 5-HT2A receptors. Acta Pol Pharm. 2004 Mar-Apr;61(2):139-50.
Part III.. 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. |
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