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: We have developed a novel fluorine-18 radiotracer, dipeptide 1 , radiolabeled in two steps from mesylate 3 . The initial radiolabeling is achieved in a short reaction time (10 min) and purified through solid-phase extraction (SPE) with modest radiochemical yields (rcy = 10 ± 2%, n = 5) in excellent radiochemical purity (rcp &gt; 99%, n = 5). The de-protection of the tert -butyloxycarbonyl (Boc) and trityl group was achieved with mild heating under acidic conditions to provide 18 F-tagged dipeptide 1 . Preliminary analysis of 18 F-dipeptide 1 was performed to confirm uptake by peptide transporters (PepTs) in human pancreatic carcinoma cell lines Panc1, BxPC3, and ASpc1, which are reported to express the peptide transporter 1 (PepT1) . Furthermore, we confirmed in vivo uptake of 18 F-dipeptide tracer 1 using microPET/CT in mice harboring subcutaneous flank Panc1, BxPC3, and Aspc1 tumors. In conclusion, we have established the radiolabeling of dipeptide 1 with fluoride-18, and demonstrated its potential as an imaging agent which may have clinical applications for the diagnosis of pancreatic carcinomas.

The Radiolabeling of a Gly-Sar Dipeptide Derivative with Flourine-18 and Its Use as a Potential Peptide Transporter PET Imaging Agent