使用单光子发射计算机断层扫描（SPECT）开发用于心脏β-肾上腺素能受体成像的放射性配体。第一部分：五种新型含碘β-肾上腺素能受体拮抗剂衍生物的不对称合成及结构表征

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

作者信息

van den Bos J C, van Doremalen P A, Dubois E A, Somsen G A, Vekemans J A, Janssen A G, Boer G J, Pfaffendorf M, van Royen E A, van Zwieten P A

机构信息

Eindhoven University of Technology, The Netherlands.

出版信息

Nucl Med Biol. 1997 Jan;24(1):1-7. doi: 10.1016/s0969-8051(96)00154-0.

DOI:10.1016/s0969-8051(96)00154-0

PMID:9080468

Abstract

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-[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.

摘要

描述了一系列碘化β-肾上腺素能受体配体的不对称合成。一种配体，(S)-(-)-[1-(2-碘苯氧基)]-3'-(叔丁基氨基)-2'-丙醇（CYBL3），基于β-肾上腺素能受体拮抗剂喷布洛尔。其他配体是β-肾上腺素能受体拮抗剂CGP12177的N-碘代乙烯基和N-碘代芳基类似物。这些已由2-氨基-3-硝基苯酚合成。此外，通过在过氧化氢存在下使用[123I]-NaI对相应的三烷基锡前体进行放射性标记，制备了放射性碘化的[123I]CYBL3和123I-[4-(3'-(1",1"-二甲基-3"-碘-2"丙烯基氨基)-2'-羟基丙氧基)]-苯并咪唑-2-酮。