TY - JOUR
AU - Stoll, T.
AU - Ermert, J.
AU - Oya, S.
AU - Kung, H. F.
AU - Coenen, H. H.
TI - Application of n.c.a. 4-[18F]fluorophenol in diaryl ether syntheses of 2-(4-[18F]fluorophenoxy)-benzylamines
JO - Journal of labelled compounds and radiopharmaceuticals
VL - 47
IS - 7
SN - 0362-4803
CY - New York, NY [u.a.]
PB - Wiley
M1 - PreJuSER-29865
SP - 443 - 455
PY - 2004
N1 - Record converted from VDB: 12.11.2012
AB - 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.
KW - J (WoSType)
LB - PUB:(DE-HGF)16
UR - <Go to ISI:>//WOS:000222499000006
DO - DOI:10.1002/jlcr.828
UR - https://juser.fz-juelich.de/record/29865
ER -