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

• Automated synthesis of [18F]FBPA was developed via reaction of BPA with [18F]F2.
• [18F]FBPA was obtained with a RCY of 8.5±2.0%.
• Nucleophilic synthesis module was adapted for electrophilic [18F]fluorinations.
• Modified synthesis module may also enable other electrophilic [18F]fluorinations.

We modified a commercially available synthesis module for nucleophilic [18F]fluorinations (TRACERlabTM FXFDG, GE Healthcare) to enable the reliable synthesis of 2-[18F]fluoro-4-borono-l-phenylalanine ([18F]FBPA) via direct electrophilic substitution of 4-borono-l-phenylalanine with [18F]F2 gas. [18F]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 [18F]radiopharmaceuticals via electrophilic substitution reactions while still being suitable for nucleophilic substitution reactions.

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