Synthesis of new hexahydro- and octahydropyrido[1,2-c]pyrimidine derivatives with an arylpiperazine moiety as ligands for 5-HT1A and 5-HT2A receptors. 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.
Herold
Fraciszek
F
Department of Drug Technology, Faculty of Pharmacy, The Medical University of Warsaw, Warsaw, Poland.
Król
Marek
M
Kleps
Jerzy
J
D008024:Ligands; D010879:Piperazines / Q000138:chemical synthesis / Q000378:metabolism; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000378:metabolism*; D044282:Receptor, Serotonin, 5-HT1A / Q000378:metabolism*; D044402:Receptor, Serotonin, 5-HT2A / Q000378:metabolism*
D008024:Ligands; D010879:Piperazines; D011743:Pyrimidines; D044402:Receptor, Serotonin, 5-HT2A; C483405:octahydropyrido(1,2-c)pyrimidine; D044282:Receptor, Serotonin, 5-HT1A