One-pot synthesis of high molar activity 6-[18F]fluoro-l-DOPA by Cu-mediated fluorination of a BPin precursor.
Andrew V MossineSean S TanzeyAllen F BrooksKatarina J MakaravageNaoko IchiishiJason M MillerBradford D HendersonMarc B SkaddanMelanie S SanfordPeter J H ScottPublished in: Organic & biomolecular chemistry (2019)
A one-pot two-step synthesis of 6-[18F]fluoro-l-DOPA ([18F]FDOPA) has been developed involving Cu-mediated radiofluorination of a pinacol boronate ester precursor. The method is fully automated, provides [18F]FDOPA in good activity yield (104 ± 16 mCi, 6 ± 1%), excellent radiochemical purity (>99%) and high molar activity (3799 ± 2087 Ci mmol-1), n = 3, and has been validated to produce the radiotracer for human use.