Scholarlink

Background <p>[<sup>11</sup>C]Phosgene is a known but underutilised labelling synthon in PET-tracer development. The production of [<sup>11</sup>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 [<sup>11</sup>C]phosgene from [<sup>11</sup>C]CO<sub>2</sub> was developed to solve issues restricting the use of [<sup>11</sup>C]phosgene. The high molar activity [<sup>11</sup>C]phosgene was then used for the labelling of biologically important molecules as a proof of concept.</p> Results <p>[<sup>11</sup>C]Phosgene was synthesized from [<sup>11</sup>C]CO by UV-mediated photochemical chlorination with chlorine gas. [<sup>11</sup>C]CO was produced by the fluoride-activated disilane reduction of cyclotron-produced [<sup>11</sup>C]CO<sub>2</sub>. [<sup>11</sup>C]Phosgene was produced with satisfactory radiochemical yield (13 ± 1&#xa0;GBq at EOS, 30 ± 4% dc. to SOS) based on [<sup>11</sup>C]CO<sub>2</sub> and molar activity of 249 ± 40&#xa0;GBq/µmol at EOS (n = 3). The radiosynthesis time was approximately 20&#xa0;min.</p> Conclusion <p>A robust synthesis route for production of high molar activity [<sup>11</sup>C]phosgene from [<sup>11</sup>C]CO<sub>2</sub> was developed. The simplicity and mild reaction conditions of the [<sup>11</sup>C]CO production method used eliminate the previous issues with Zn-based reduction of [<sup>11</sup>C]CO<sub>2</sub>. Intermediate purification of [<sup>11</sup>C]CO guaranteed efficient [<sup>11</sup>C]phosgene production, and removal of unreacted Cl<sub>2</sub> 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.</p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

High molar activity [11C]phosgene from [11C]CO2

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2026年7月24日

查看全文
  • Edla Kerminen,
  • Thomas Keller,
  • Simo Salo,
  • Johan Rajander,
  • Olof Solin,
  • Anna Krzyczmonik,
  • Anna K. Kirjavainen

摘要

Background

[11C]Phosgene is a known but underutilised labelling synthon in PET-tracer development. The production of [11C]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 [11C]phosgene from [11C]CO2 was developed to solve issues restricting the use of [11C]phosgene. The high molar activity [11C]phosgene was then used for the labelling of biologically important molecules as a proof of concept.

Results

[11C]Phosgene was synthesized from [11C]CO by UV-mediated photochemical chlorination with chlorine gas. [11C]CO was produced by the fluoride-activated disilane reduction of cyclotron-produced [11C]CO2. [11C]Phosgene was produced with satisfactory radiochemical yield (13 ± 1 GBq at EOS, 30 ± 4% dc. to SOS) based on [11C]CO2 and molar activity of 249 ± 40 GBq/µmol at EOS (n = 3). The radiosynthesis time was approximately 20 min.

Conclusion

A robust synthesis route for production of high molar activity [11C]phosgene from [11C]CO2 was developed. The simplicity and mild reaction conditions of the [11C]CO production method used eliminate the previous issues with Zn-based reduction of [11C]CO2. Intermediate purification of [11C]CO guaranteed efficient [11C]phosgene production, and removal of unreacted Cl2 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.