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
- 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.
Publication date
January 1997
DOIAbstract
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.<br/
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