Fluorine‐18 labelling of a series of potential EGFRvIII targeting peptides with a parallel labelling approach using [18F]FPyME

There is growing interest in the use of radiolabelled peptides as receptor targeting agents for diagnostic imaging of various cancer types using positron emission tomography. In this work, 1‐3‐(2‐¹⁸F]fluoropyridin‐3‐yloxy)propyl]pyrrole‐2,5‐dione (¹⁸F]FPyME) has been used for parallel fluorine‐18 labelling of PEPHC1, a peptide selective towards the cancer‐specific mutation of the epidermal growth factor receptor (EGFRvIII), and a number of truncated and mutated analogues. Conjugation of the peptides with ¹⁸F]FPyME was achieved within 10 min in non‐decay‐corrected radiochemical yields of 30–50%. The high yield of the conjugation reaction combined with its short synthesis time allows the labelling of several peptides from a single batch of ¹⁸F]FPyME. Copyright © 2010 John Wiley & Sons, Ltd.