Tos-Nos-Mos: Synthesis of different aryl sulfonate precursors for the radiosynthesis of the alpha7 nicotinic acetylcholine receptor radioligand [(18)F]NS14490.

Authors :: Rötering S
Scheunemann M
Günther R
Löser R
Hiller A
Dan Peters
Brust P
Fischer S
Steinbach J
Source :: Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine [Appl Radiat Isot] 2016 Aug; Vol. 114, pp. 57-62. Date of Electronic Publication: 2016 Apr 28.
Publication Year :: 2016
Abstract: Radiopharmacological investigations of [(18)F]NS14490 have proven that this radiotracer could be a potential PET radiotracer for imaging of alpha7 nicotinic acetylcholine receptor particularly with regard to vulnerable plaques of diseased vessels. For further optimisation of the previously automated one-pot radiosynthesis of [(18)F]NS14490 using a tosylate precursor, precursors with other leaving groups (nosylate and mosylate) were synthesized and compared with the tosylate with respect to their reactivities towards [(18)F]fluoride. The use of these different precursors resulted in comparable labelling yields of [(18)F]NS14490. A novel mosylate precursor was synthesized and evaluated, which has revealed a higher stability during a storage period of five months compared to the corresponding tosylate and nosylate.<br /> (Copyright © 2016. Published by Elsevier Ltd.)

Language :: English
ISSN :: 1872-9800
Volume :: 114
Database :: MEDLINE
Journal :: Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine
Publication Type :: Academic Journal
Accession number :: 27183376
Full Text :: https://doi.org/10.1016/j.apradiso.2016.04.028

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