Development of radioligands for the imaging of cardiac beta-adrenoceptors using SPECT .1. Asymmetric synthesis and structural characterization of five new iodine-containing beta-adrenoceptor antagonist derivatives

Autor: van den Bos, J.C., van Doremalen, P.A.P.M., Dubois, E.A., Somsen, G.A., Vekemans, J.A.J.M., Janssen, A.G.M., Boer, G.J., Pfaffendorf, M., van Royen, E.A., van Zwieten, P.A.
Přispěvatelé: Applied Physics and Science Education, Macromolecular and Organic Chemistry, Chemical Engineering and Chemistry
Jazyk: angličtina
Rok vydání: 1997
Předmět:
Zdroj: Nuclear Medicine and Biology, 24(1), 1-7. Elsevier
ISSN: 0969-8051
Popis: The asymmetric synthesis of a series of iodinated beta-adrenoceptor ligands is described. One ligand, (S)-(-)-[1-(2-iodophenoxy)]-3'-(tert-butylamino)-2'-propanol (CYBL3), is based on the beta-adrenoceptor antagonist penbutolol. The other ligands are N-iodovinyl and N-iodoaryl analogues of the beta-adrenoceptor antagonist CGP12177. These have been synthesized from 2-amino-3-nitrophenol. Furthermore, radioiodinated [123I]CYBL3 and [123I](2'S,2"E)-[4-(3'-(1",1"-dimethyl-3"-iodo-2" propenylamino)-2'-hydroxy propoxy)]-benzimidazol-2-one have been prepared by radiolabelling the corresponding trialkyltin precursors using [123I]-NaI in the presence of hydrogen peroxide.
Databáze: OpenAIRE
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