High molar activity [11C]phosgene from [11C]CO2
[ 11 C]Phosgene is a known but underutilised labelling synthon in PET-tracer development. The production of [ 11 C]phosgene faces many problems such as difficulties in achieving high molar activity, regular key component replacement and complexity of the synthesis, thereby hindering its wider use. In this paper, a robust and semi-automated synthesis route for production of [ 11 C]phosgene from [ 11 C]CO 2 was developed to solve issues restricting the use of [ 11 C]phosgene. The high molar activity [ 11 C]phosgene was then used for the labelling of biologically important molecules as a proof of concept. [ 11 C]Phosgene was synthesized from [ 11 C]CO by UV-mediated photochemical chlorination with chlorine gas. [ 11 C]CO was produced by the fluoride-activated disilane reduction of cyclotron-produced [ 11 C]CO 2 . [ 11 C]Phosgene was produced with satisfactory radiochemical yield (13 ± 1 GBq at EOS, 30 ± 4% dc. to SOS) based on [ 11 C]CO 2 and molar activity of 249 ± 40 GBq/µmol at EOS (n = 3). The radiosynthesis time was approximately 20 min. A robust synthesis route for production of high molar activity [ 11 C]phosgene from [ 11 C]CO 2 was developed. The simplicity and mild reaction conditions of the [ 11 C]CO production method used eliminate the previous issues with Zn-based reduction of [ 11 C]CO 2 . Intermediate purification of [ 11 C]CO guaranteed efficient [ 11 C]phosgene production, and removal of unreacted Cl 2 minimised unwanted side reactions. This method utilises a fixed-line device with simple set up and mild conditions. With this method, it is possible to perform syntheses reliably with good radiochemical yields and high molar activities in a short synthesis time.
Authors
- Johan Rajander (ORCID: https://orcid.org/0000-0003-3591-0963)
- Anna Krzyczmonik
- Olof Solin
- Simo Salo
- Edla Kerminen
- Anna K. Kirjavainen
- Thomas Keller
Institutions
- Åbo Akademi University (FI)
- University of Turku (FI)
- National Centre for Nuclear Research (PL)
- Turku PET Centre (FI)
Publication Details
- Journal
- EJNMMI Radiopharmacy and Chemistry
- Published
- 2026-07-24
- DOI
- https://doi.org/10.1186/s41181-026-00472-w
- Primary Topic
- Radiopharmaceutical Chemistry and Applications
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- Luonnontieteiden ja Tekniikan Tutkimuksen Toimikunta