Startseite Towards automated solid phase radiofluorination for dose-on-demand PET: retention of activity by solid support
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Towards automated solid phase radiofluorination for dose-on-demand PET: retention of activity by solid support

  • Bente Mathiessen , Gregory Severin und Fedor Zhuravlev EMAIL logo
Veröffentlicht/Copyright: 28. Januar 2015

Abstract

On-column [18F]fluoride trapping and radiofluorination of 2-(naphthalen-1-yl)ethyl-4-methylbenzenesulfonate (C10H7(CH2)2OTs), performed on polystyrene supported phosphazene base PS-P2tBu yielded [18F]1-(2-fluoroethyl)naphthalene ([18F]C10H7(CH2)2F) in 50% radiochemical yield but left up to 43% of activity unreacted on the resin. This activity could be eluted with Kryptofix/K2CO3 and then used for conventional radiofluorination of the same substrate, suggesting that the column-retained activity was present in the form of [18F]fluoride entrapped in polymer matrix. An approach to minimize the amount of entrapped [18F]fluoride by use of glass beads functionalized with alkylsilane-derivatized phosphazene residues was attempted but was stymied by fluorolysis/hydrolysis of the alkylsilane spacer. The results suggest that the key to high yield of on-column radiofluorination is to minimize the residual [18F]fluoride absorption in the matrix by the judicious choice of solid support.

Received: 2014-2-25
Accepted: 2014-12-17
Published Online: 2015-1-28
Published in Print: 2015-3-28

©2015 Walter de Gruyter Berlin/Boston

Heruntergeladen am 20.10.2025 von https://www.degruyterbrill.com/document/doi/10.1515/ract-2014-2370/html
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