4.7 Article

Cross-coupling of [11C]methyllithium for 11C-labelled PET tracer synthesis

Journal

CHEMICAL COMMUNICATIONS
Volume 57, Issue 2, Pages 203-206

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/d0cc05392a

Keywords

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Funding

  1. Netherlands Organization for Scientific Research
  2. Royal Netherlands Academy of Arts and Sciences (KNAW)
  3. Ministry of Education, Culture and Science [024.60 1035]

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This study presents the cross-coupling of aryl bromides with [C-11]CH3Li for labelling various tracers for PET imaging. The radiolabelled products were obtained in high yields at room temperature and short reaction times, compatible with the short half-life of C-11. Investigating the automation of this protocol on a synthesis module is seen as a crucial step towards a rapid method for synthesizing C-11-labelled compounds for PET imaging.
The cross-coupling of aryl bromides with [C-11]CH3Li for the labelling of a variety of tracers for positron emission tomography (PET) is presented. The radiolabelled products were obtained in excellent yields, at rt and after short reaction times (3-5 min) compatible with the half-life of C-11 (20.4 min). The automation of the protocol on a synthesis module is investigated, representing an important step towards a fast method for the synthesis of C-11-labelled compounds for PET imaging.

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