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Radiochemistry

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Contact :  Radiochem-MIRCen@cea.fr

Published on 3 July 2024

MIRCen's radiochemistry platform allows the development and the production of new radiotracers labeled with positron emitters. These very sensitive molecules are at the basis for PET imaging.

 The IBA Cyclone 18/18 cyclotron enables the production of two short half-life radioisotopes, the carbon-11 and the fluor-18 (respectively 20.4 et 109.8 min), in the form of  [11C]CO2 and [18F]fluoride. In the near future, a third radioisotope will be produced, the zirconium-89. Its half-life of 3.3 days is well suited for imaging macromolecules such as antibodies.


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IBA Cyclone 18/18 cyclotron*


Activities

Carbon-11 labeling: 11C-methylation from [11C]MeI and [11C]MeOTf production of [11C]CO and of [11C]HCN, 11C-carbonylations, 11C-cyanations,11C-catalyses au Pd, Rh, Se et Ni, aryl et alkyl-11C-methylations photocatalyzed (using the method of Pipal et al, 589 (7843), 542-547, Nature 2021)...

Complex multistep syntheses, e.g. the ligand for D2/D3 receptors, the (+)[11C]PHNO (Plisson et al, 70, 380-387, Appl Radiat Isot 2012).

Fluor-18 labeling: direct aromatic or aliphatic nucleophilic 18F-fluorination, indirect markings of macromolecules (synthesis of a prosthetic group followed by coupling of the group with the macromolecule under mild reaction conditions). It is also possible to use « Click » chemistry methods.

Complex multistep syntheses are possible with 4 possibilities of pre-purification, 2 radio-HPLC and 2 reformulation systems of the automat.



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Example of a labeling using 2 reactors and 2 HPLC : synthesis and purification of 2-[18F]fluoroethyl tosylate followed by the S-18F-fluoroethylation of a thiophosphate (Vries et al, 58, 469-476, Appl Radiat Isot 2003)

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Example of a labeling using 2 reactors and 2 HPLC : synthesis and purification of 2-[18F]fluoroethyl tosylate followed by the S-18F-fluoroethylation of a thiophosphate (Vries et al, 58, 469-476, Appl Radiat Isot 2003)


Principal equipments 

  • Cyclone 18/18 Cyclotron (IBA)
  • Hot cell (Lemer Pax) for labeling and sampling at the end of the radiosynthesis.
  • Automated synthesis system MeIplus Research (Synthra) for production of carbon-11 labeled compounds; equipped with a photoreactor (450 nm).
  • Automated synthesis system FlexLab (iPhase) for production of fluor-18 labeled compounds; equipped with 4 reactors (each can be heated or cooled).
  • Analytical Radio-HPLC (Waters / Berthold) (e2695, Empower 3 / Herm fLumo).

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Hot cells, Lemer Pax*


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Automated synthesis system, MeIplus Research, Synthra
MeIplus Research synoptic



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Automated synthesis system, FlexLab, iPhase
FlexLab synoptic



* crédit photos : L.Godart/CEA