[ 11 C]phosgene: Synthesis and application for development of PET radiotracers.

Autor: Fukumura T; Department of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan., Mori W; Department of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan., Ogawa M; Department of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan; SHI Accelerator Service, Ltd., Tokyo 141-8686, Japan., Fujinaga M; Department of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan., Zhang MR; Department of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan. Electronic address: zhang.ming-rong@qst.go.jp.
Jazyk: angličtina
Zdroj: Nuclear medicine and biology [Nucl Med Biol] 2021 Jan; Vol. 92, pp. 138-148. Date of Electronic Publication: 2020 May 01.
DOI: 10.1016/j.nucmedbio.2020.04.007
Abstrakt: Carbon-11-labeled phosgene ([ 11 C]phosgene, [ 11 C]COCl 2 ) is a useful labeling agent that connects two heteroatoms by inserting [ 11 C]carbonyl ( 11 C=O) function in carbamates, ureas, and carbonates, which are components of biologically important heterocyclic compounds and functional groups in drugs as a linker of fragments with in vivo stability. Development of 11 C-labeled PET tracers has been performed using [ 11 C]phosgene as a labeling agent. However, [ 11 C]phosgene has not been frequently used for 11 C-labeling because preparation of [ 11 C]phosgene required dedicated synthesis apparatus (not commercially available) and had problems in reproducibility and reliability. In our laboratory, an improved method for synthesizing [ 11 C]phosgene using a carbon tetrachloride detection tube kit in environmental air analysis and the automated synthesis system for preparing [ 11 C]phosgene have been developed in 2009. This apparatus has been used for routine synthesis of 11 C-labeled tracers 1-4 times/week. Using [ 11 C]phosgene we have developed and produced many PET radiotracers containing [ 11 C]urea and [ 11 C]carbamate moieties. In this review, we report the performance of our method for preparing [ 11 C]phosgene, including automated synthesis apparatus developed in house, and the application of [ 11 C]phosgene for development and production of 11 C-labeled PET tracers.
(Copyright © 2020 Elsevier Inc. All rights reserved.)
Databáze: MEDLINE
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