Development of radioligands for the imaging of cardiac β-adrenoceptors using SPECT. Part I: Asymmetric synthesis and structural characterization of five new iodine-containing β-adrenoceptor antagonist derivatives
The asymmetric synthesis of a series of iodinated β-adrenoceptor ligands is described. One ligand, (S)-(−)-[1-(2-iodophenoxy)]-3′-( tert-butylamino)-2′-propanol (CYBL3), is based on the β-adrenoceptor antagonist penbutolol. The other ligands are N-iodovinyl and N-iodoaryl analogues of the β-adrenoce...
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Veröffentlicht in: | Nuclear medicine and biology 1997, Vol.24 (1), p.1-7 |
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Hauptverfasser: | , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | The asymmetric synthesis of a series of iodinated β-adrenoceptor ligands is described. One ligand, (S)-(−)-[1-(2-iodophenoxy)]-3′-(
tert-butylamino)-2′-propanol (CYBL3), is based on the β-adrenoceptor antagonist penbutolol. The other ligands are
N-iodovinyl and
N-iodoaryl analogues of the β-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. |
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ISSN: | 0969-8051 1872-9614 |
DOI: | 10.1016/S0969-8051(96)00154-0 |