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One pot radiofluorination of a new potential PSMA ligand [Al 18 F]NOTA‐DUPA‐Pep
Author(s) -
Malik Noeen,
Zlatopolskiy Boris,
Machulla HansJuergen,
Reske Sven N,
Solbach Christoph
Publication year - 2012
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2944
Subject(s) - chemistry , radiosynthesis , yield (engineering) , ligand (biochemistry) , specific activity , in vivo , combinatorial chemistry , radiochemistry , glutamate carboxypeptidase ii , kinetics , labelling , stereochemistry , enzyme , organic chemistry , biochemistry , prostate , receptor , medicine , materials science , microbiology and biotechnology , physics , cancer , quantum mechanics , metallurgy , biology
Up to now, many radiolabeled ligands targeting prostate‐specific membrane antigen (PSMA) have been synthesized. To carry out radiofluorinations, there have been several approaches mainly involving two steps of radiosynthesis. However, in case of labelings with high activities, one radiosynthetic step (‘one pot synthesis’) is highly desirable. As an alternative, radiofluorinations of peptides coupled to the NOTA complex via Al 18 F appear to be very promising, both in terms of feasible labelling procedure and stability in vivo . Therefore, in the present study, we synthesized a new PSMA‐ligand, that is, NOTA‐DUPA‐Pep, labeled with Al 18 F and examined the reaction kinetics in dependence on temperature, time, concentration of precursor, and AlCl 3 solution. Highest radiochemical yields of 83 ± 1.1% were obtained at 105 °C after 15 min of reaction time. At the end of synthesis, [Al 18 F]NOTA‐DUPA‐Pep was prepared with a radiochemical purity of ≥98% with an overall yield of 79 ± 0.7% ( n = 3) (decay uncorrected) within 55 min. Copyright © 2012 John Wiley & Sons, Ltd.