Automated electrophilic radiosynthesis of [18F]FBPA using a modified nucleophilic GE TRACERlab FXFDG. (October 2015)

• Record Type: Journal Article
• Authors: Mairinger, Severin; Stanek, Johann; Wanek, Thomas; Langer, Oliver; Kuntner, Claudia
• Is Part Of: Applied radiation and isotopes. Volume 104(2015:Oct.)
• Page Start: 124
• Page End: 127
• Publication Date: 2015-10
• Subjects: 2-[18F]fluoro-4-borono-l-phenylalanine -- Boron neutron capture therapy -- Automated synthesis -- TRACERlab™ FXFDG -- Electrophilic [18F]fluorination; Radiology -- Periodicals; Radiation -- Industrial applications -- Periodicals; Nuclear chemistry -- Periodicals; Internet resource; Periodical; 660.298
• DOI: 10.1016/j.apradiso.2015.06.034
• Languages: English
• ISSNs: 0969-8043

Abstract

Abstract: We modified a commercially available synthesis module for nucleophilic [ 18 F]fluorinations (TRACERlab TM FXFDG, GE Healthcare) to enable the reliable synthesis of 2-[ 18 F]fluoro-4-borono-l -phenylalanine ([ 18 F]FBPA) via direct electrophilic substitution of 4-borono-l -phenylalanine with [ 18 F]F2 gas. [ 18 F]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 [ 18 F]radiopharmaceuticals via electrophilic substitution reactions while still being suitable for nucleophilic substitution reactions. Graphical abstract: Highlights: Automated synthesis of [ 18 F]FBPA was developed via reaction of BPA with [ 18 F]F2 . [ 18 F]FBPA was obtained with a RCY of 8.5±2.0%. Nucleophilic synthesis module was adapted for electrophilic [ 18 F]fluorinations. Modified synthesis module may also enable other electrophilic [ 18 F]fluorinations.