Fully automated preparation and conjugation of N-succinimidyl 4-[18F]fluorobenzoate ([18F]SFB) with RGD peptide using a GE FASTlab™ synthesizer.
OBJECTIVE
The aim of this work was to automate the radiosynthesis of [(18)F]SFB, a widely used reagent for the labeling of biomolecules with (18)F on a new generation commercial synthesis module (FASTLab™, GE Healthcare).


METHODS
Two synthesis approaches were implemented on this module: the classical "two-pot radiosynthesis" and the more recently described "one-pot" method.


RESULTS
The "two-pot" approach affords [(18)F]SFB with a 42% decay-corrected yield in 57 min (n = 24) with a chemical purity sufficient to avoid an intermediate HPLC purification. The recently established "one-pot" method, afforded a product with a lower chemical purity, in the conditions used in this report. The lower d.c. yield obtained (32% (n = 15)) was related to the low (18)F labeling yields obtained in MeCN compared with DMSO. The subsequent conjugation step with a RGD (PRGD2) peptide was also successfully automated.


CONCLUSIONS
The formulated [(18)F]FPRGD2 was obtained without any operator manipulation with a d.c. yield of 13% ± 3% (n = 13) in 130 min, a radiochemical purity >98% and a specific activity of 140 ± 40 TBq/mmol.
Cyclotron Research Center, Liege University, Liege, Belgium. dthonon@ulg.ac.be
David
D
Thonon
David
D
Goblet
Eve
E
Goukens
Geoffroy
G
Kaisin
Jérôme
J
Paris
Joël
J
Aerts
Steve
S
Lignon
Xavier
X
Franci
Roland
R
Hustinx
André
A
Luxen
D001331:Automation; D001565:Benzoates / Q000138:chemical synthesis* / Q000737:chemistry; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000737:chemistry; D011854:Radiochemistry / Q000295:instrumentation* / Q000379:methods*; D013388:Succinimides / Q000138:chemical synthesis* / Q000737:chemistry
D001565:Benzoates; D005462:Fluorine Radioisotopes; D009842:Oligopeptides; D013388:Succinimides; C075713:N-succinimidyl-4-fluorobenzoate; C047981:arginyl-glycyl-aspartic acid
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