B Academy of Molecular Imaging and Society for Molecular Imaging, 2011 Published Online: 26 January 2011 DOI: 10.1007/s11307-011-0470-x Mol Imaging Biol (2011) 13:1088Y1095 RESEARCH ARTICLE Fully Automated Preparation and Conjugation of N-Succinimidyl 4-[ 18 F]Fluorobenzoate ([ 18 F]SFB) with RGD Peptide Using a GE FASTlab™ Synthesizer David Thonon, 1 David Goblet, 1 Eve Goukens, 1 Geoffroy Kaisin, 1 Jérôme Paris, 1 Joël Aerts, 1 Steve Lignon, 2 Xavier Franci, 2 Roland Hustinx, 3 André Luxen 1 1 Cyclotron Research Center, Liege University, Sart-Tilman B. 30, 4000, Liege, Belgium 2 GE Healthcare-MDX PET Chemistry Systems, 10/2, rue Marie Curie, 4431, Loncin, Belgium 3 Division of Nuclear Medicine, University Hospital of Liège, Liège, Belgium Abstract Purpose: 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). Procedures: 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 998% and a specific activity of 140±40 TBq/mmol. Key words: N-Succinimidyl 4-[ 18 F]fluorobenzoate, [ 18 F]SFB, [ 18 F]Fluorobenzoic acid, [ 18 F]FBA, Dimeric RGD peptide, Fluorine-18, Positron emission tomography, PET, GE FASTlab™, Radiosynthesis automation Introduction N -Succinimidyl 4-[ 18 F]fluorobenzoate ([ 18 F]SFB) 4 has been widely used for labeling of biomolecules. For example, annexin V, the anti-granulocyte antibody BW 250/ 183 (anti-CD66), cyclic RGD-peptides, α-MSH, and neuro- tensin have been labeled with this reagent [1–7]. The initially laborious and time-consuming radiosynthesis of [ 18 F]SFB 4 has been improved over the years making it more suitable for clinical applications. In particular, the radiosynthesis of [ 18 F]SFB has been automated by several groups. Mäding et al. reported module-assisted synthesis of [ 18 F]SFB using the TRACER- lab FX FDG with decay-corrected (d.c.) yields in the range of 34–38% in 68 min [8]. Using a Siemens/CTI chemistry process control unit (CPCU), Marik obtained d.c. yields of 46% in 78 min [9]. Finally, in 2008, Johnstöm et al. Correspondence to: David Thonon; e-mail: dthonon@ulg.ac.be