Fully Automated Preparation and Conjugation of N-Succinimidyl 4-[18F]Fluorobenzoate ([18F]SFB) with RGD Peptide Using a GE FASTlab™ Synthesizer

Abstract

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.

Synthesis and Biologic Evaluation of Novel 18F-Labeled Probes Targeting Prostate-Specific Membrane Antigen for PET of Prostate Cancer

“…However, the radiochemical yield of 18 F-DCFPyL is low (2.8% 6 1.2%) (18). To overcome this disadvantage, we designed novel PSMA-targeting probes using 18 F-SFB, which has been obtained with a high radiochemical yield using the automated facile synthesis (20)(21)(22)(23)(24)(25). The design of these novel PSMA imaging probes was based on the results of our previous study.…”

“…This compound, however, has a low radiochemical yield (2.8% 6 1.2%) (18). Recently, an 18 F-labeling reagent, 18 F-SFB, with high radiochemical yield, obtained using automated facile synthesis has become available (20)(21)(22)(23)(24)(25). Thus, we decided to design novel PSMA-targeted probes labeled with 18 F-SFB.…”

18F-FPRGD2 PET/CT Imaging of Integrin αvβ3 in Renal Carcinomas: Correlation with Histopathology

“…The 18 F-FPRGD2 was produced using a published method in compliance with current good manufacturing practice regulations (2). The 18 F-FPRGD2 radiosynthesis process and the 18 F-FPRGD2 PET/CT acquisition parameters are described in the supplemental data (supplemental materials are available at http://jnm.…”

Silicon-[18F]Fluorine Radiochemistry: Basics, Applications and Challenges

“…Therefore, 18 F-labeling reactions of peptides normally imply multistep syntheses consisting of the production of a secondary labeling precursor bearing the F-18 label, which has then to be reacted with the peptide. Although the synthesis of several secondary labeling precursors has been improved in recent years, yielding the labeled peptides in high yields and relatively short reaction times, the multi-step syntheses of 18 F-labeled peptides using these synthons still require long preparation times-which is unfavorable, considering the short half-life of 18 F-as well as complex and costly in terms of technical equipment [34][35][36].…”