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1 PublicationN-Arylation of indoles with 4-[18F]fluoroiodobenzene: synthesis of 18F-labelled σ2 receptor ligands for positron emission tomography (PET)
Wüst, F.; Knieß, T.
Abstract
Summary: The palladium-mediated N-arylation of indoles with 4-[18F]fluoroiodobenzene as a novel radiolabelling method has been developed. Optimized reaction conditions were elaborated by variation of different catalyst systems (CuI/1,2-diamines and Pd2(dba)3/phosphine ligands), based and solvents in the reaction of indole with 4-[18F]fluoroiodobenzene. Optimized reaction conditions (Pd2(dba)3/(2-(dicyclohexyl-phosphino)-2´-(N,N-dimethylamino)-biphenyl, NaOBut, toluene, 100 °C for 20 min) were applied for the synthesis of 18F-labelled σ2 receptor ligands [18F]-11 and [18F]-13 which were obtained in 91 and 84 % radiochemical yields, respectively.
Keywords: N-arylation; 4-[18F]fluoroiodobenzene; σ2 ligands
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Journal of Labelled Compounds and Radiopharmaceuticals 48(2005), 31-43
DOI: 10.1002/jlcr.893
Cited 31 times in Scopus
Permalink: https://www.hzdr.de/publications/Publ-6887