Automated electrophilic radiosynthesis of [18F]FBPA using a modified nucleophilic GE TRACERlab FXFDG

We modified a commercially available synthesis module for nucleophilic [F-18]fluorinations (TRACERlab (TM) FXFDG, GE Healthcare) to enable the reliable synthesis of 2-[F-18]fluoro-4-borono-L-phenylalanine ([F-18]FBPA) via direct electrophilic substitution of 4-borono-L-phenylalanine with [F-18]F-2 gas. [F-18]FBPA was obtained with a RCY of 8.5 +/- 2.0% and a radiochemical purity of 98 +/- 1% in a total synthesis time of 72 +/- 7 min (n=22). The modified synthesis module might also be useful for the synthesis of other [F-18]radiopharmaceuticals via electrophilic substitution reactions while still being suitable for nucleophilic substitution reactions. (C) 2015 Elsevier Ltd. All rights reserved.