Enhanced copper-mediated (18)F-fluorination of aryl boronic esters provides eight radiotracers for PET applications.

Authors :: Preshlock S
Calderwood S
Verhoog S
Tredwell M
Huiban M
Hienzsch A
Gruber S
Wilson TC
Taylor NJ
Cailly T
Schedler M
Collier TL
Passchier J
Smits R
Mollitor J
Hoepping A
Mueller M
Genicot C
Mercier J
Gouverneur V
Source :: Chemical communications (Cambridge, England) [Chem Commun (Camb)] 2016 Jun 28; Vol. 52 (54), pp. 8361-4.
Publication Year :: 2016
Abstract: [(18)F]FMTEB, [(18)F]FPEB, [(18)F]flumazenil, [(18)F]DAA1106, [(18)F]MFBG, [(18)F]FDOPA, [(18)F]FMT and [(18)F]FDA are prepared from the corresponding arylboronic esters and [(18)F]KF/K222 in the presence of Cu(OTf)2py4. The method was successfully applied using three radiosynthetic platforms, and up to 26 GBq of non-carrier added starting activity of (18)F-fluoride.

Subjects :: Catalysis
Radioactive Tracers
Boronic Acids chemistry
Copper chemistry
Esters chemistry
Fluorine Radioisotopes
Halogenation
Positron-Emission Tomography

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