%0 Journal Article
%A Stoll, T.
%A Ermert, J.
%A Oya, S.
%A Kung, H. F.
%A Coenen, H. H.
%T Application of n.c.a. 4-[18F]fluorophenol in diaryl ether syntheses of 2-(4-[18F]fluorophenoxy)-benzylamines
%J Journal of labelled compounds and radiopharmaceuticals
%V 47
%N 7
%@ 0362-4803
%C New York, NY [u.a.]
%I Wiley
%M PreJuSER-29865
%P 443 - 455
%D 2004
%Z Record converted from VDB: 12.11.2012
%X The availability of no-carrier-added (n.c.a.) 4-[F-18]fluorophenol offers the possibility of introducing the 4-[F-18]fluorophenoxy moiety into potential radiopharmaceuticals. Besides alkyl-aryl ether synthesis using n.c.a. 4-[F-18]fluorophenol the diaryl ether coupling is an attractive synthetic method to enlarge the spectrum of interesting labelling procedures. As examples the syntheses of n.c.a. 2-(4-[F-18]fluorophenoxy)-N,N-dimethylbenzylamine and n.c.a. 2-(4-[F-18]fluorophenoxy)-N-methylbenzylamine were realized by an Ullmann ether synthesis of corresponding 2-bromobenzoic acid amides using tetrakis(acetonitrile)copper(I) hexafluorophosphate as catalyst and a subsequent reduction of the amides formed. The radiochemical yield of the coupling varied between 5 and 65% based on labelled 4-[F-18]fluorophenol. Both compounds are structural analogues of recently published radiotracers for imaging the serotonin reuptake transporter sites (SERT). However, in vitro binding assays of both molecules showed only a low affinity towards monoamine transporters. Copyright (C) 2004 John Wiley Sons, Ltd.
%K J (WoSType)
%F PUB:(DE-HGF)16
%9 Journal Article
%U <Go to ISI:>//WOS:000222499000006
%R 10.1002/jlcr.828
%U https://juser.fz-juelich.de/record/29865