Aspects on the Synthesis and Design of 11C-Tracers for PET

Långström, Bengt; Antoni, Gunnar; Andersson, Yvonne; Axelsson, Svante; Bjurling, Peter; Fasth, Karl-Johan; Gee, Anthony; Hörnfeldt, Katarina; Kihlberg, Tor; Westerberg, Göran; Watanabe, Yasuyoshi

doi:10.1007/978-1-4899-0626-7_4

Cited by 2 publications

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“…Special synthetic methods are required for the production of PET tracers because of the short half-lives and the submicromole quantities involved . Development of new 11 C-labeled precursors and new synthetic labeling strategies is important not only to increase the number of compounds that can be labeled but also to give the option to label a given compound in selected positions . Throughout the development of a synthetic labeling method using short-lived radionuclides, the recognition of time as a parameter in the same category as chemical yield is important …”

Section: Introductionmentioning

confidence: 99%

[¹¹C]Carbon Monoxide in Selenium-Mediated Synthesis of ¹¹C-Carbamoyl Compounds

2002

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Using either amines, amino alcohols, or alcohols in selenium-mediated synthesis with [(11)C]carbon monoxide, 3 ureas, 6 carbamates, and 1 carbonate were labeled. Tetrabutylammonium fluoride ((TBA)F) was discovered to form a soluble and reactive complex with selenium and drastically increase the radiochemical yields. Of the selected carbamoyl compounds, one was a receptor ligand, one was an enzyme inhibitor, and one was a muscular relaxant pharmaceutical. The (11)C-target compounds were obtained in radiochemical yields ranging from low to almost quantitative and with specific radioactivity up to 1300 GBq/micromol. The radiochemical purity of the final products exceeded 98%. In one case, the corresponding (13)C-substituted compound was produced to verify the position of the (11)C-label. In a typical experiment starting with 16.4 GBq [(11)C]carbon monoxide, 7.0 GBq of LC-purified 5-phenyl-1,3-oxazolidin-[2-(11)C]-2-one was obtained within 20 min from start of the carbonylation reaction (84% decay-corrected radiochemical yield). The presented approach is an interesting alternative to the use of [(11)C]phosgene in labeling chemistry.

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Section: Introductionmentioning

confidence: 99%

[¹¹C]Carbon Monoxide in Selenium-Mediated Synthesis of ¹¹C-Carbamoyl Compounds

2002

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“…Special synthetic procedures are required for the production of these tracers on account of their radioactivity, short half-lives, and the submicromole quantities involved . The development of new 11 C-labeled precursors is important not only in order to increase the number of compounds that can be labeled with 11 C but also for increasing the possibility of labeling a given compound in different positions . Throughout the development of a production method, the recognition of time as a parameter in the same category as chemical yield and purity is an important consideration …”

Section: Introductionmentioning

confidence: 99%

Biologically Active ¹¹C-Labeled Amides Using Palladium-Mediated Reactions with Aryl Halides and [¹¹C]Carbon Monoxide

1999

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Using [11C]carbon monoxide in palladium-mediated synthesis, six amides were labeled with 11C. Phenyl and benzyl halides with halides as additional substituents were carbonylated and reacted with primary and secondary amines. Four of the selected amides were receptor ligands, one was a precursor to a receptor ligand, and one was a model compound. The 11C-labeled amides were obtained with good to almost quantitative radiochemical yields with specific activities up to 1000 GBq/μmol. The radiochemical purity of the final products exceeded 98%. In one case, the corresponding 13C-substituted compound was produced to verify the position of the label. In a typical experiment starting with 5.0 GBq of [11C]carbon monoxide, 2.2 GBq of LC-purified N-(2-aminoethyl)-4-chloro[carbonyl-11C]benzamide was obtained within 15 min from the start of the carbonylation reaction (74% decay-corrected radiochemical yield). The presented approach gives significant new possibilities for 11C-labeling and is seen to be valuable also for synthesis of 13C- and 14C-substituted compounds.

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Aspects on the Synthesis and Design of 11C-Tracers for PET

Cited by 2 publications

References 20 publications

[¹¹C]Carbon Monoxide in Selenium-Mediated Synthesis of ¹¹C-Carbamoyl Compounds

[¹¹C]Carbon Monoxide in Selenium-Mediated Synthesis of ¹¹C-Carbamoyl Compounds

Biologically Active ¹¹C-Labeled Amides Using Palladium-Mediated Reactions with Aryl Halides and [¹¹C]Carbon Monoxide

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Aspects on the Synthesis and Design of 11C-Tracers for PET

Cited by 2 publications

References 20 publications

[11C]Carbon Monoxide in Selenium-Mediated Synthesis of 11C-Carbamoyl Compounds

[11C]Carbon Monoxide in Selenium-Mediated Synthesis of 11C-Carbamoyl Compounds

Biologically Active 11C-Labeled Amides Using Palladium-Mediated Reactions with Aryl Halides and [11C]Carbon Monoxide

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[¹¹C]Carbon Monoxide in Selenium-Mediated Synthesis of ¹¹C-Carbamoyl Compounds

[¹¹C]Carbon Monoxide in Selenium-Mediated Synthesis of ¹¹C-Carbamoyl Compounds

Biologically Active ¹¹C-Labeled Amides Using Palladium-Mediated Reactions with Aryl Halides and [¹¹C]Carbon Monoxide