Dataset Information

Instantaneous Conversion of [¹¹ C]CO₂ to [¹¹ C]CO via Fluoride-Activated Disilane Species.

ABSTRACT: The development of a fast and novel methodology to generate carbon-11 carbon monoxide ([¹¹ C]CO) from cyclotron-produced carbon-11 carbon dioxide ([¹¹ C]CO₂ ) mediated by a fluoride-activated disilane species is described. This methodology allows up to 74?% conversion of [¹¹ C]CO₂ to [¹¹ C]CO using commercially available reagents, readily available laboratory equipment and mild reaction conditions (room temperature). As proof of utility, radiochemically pure [carbonyl-¹¹ C]N-benzylbenzamide was successfully synthesized from produced [¹¹ C]CO in up to 74?% radiochemical yield (RCY) and >99?% radiochemical purity (RCP) in ?10?min from end of [¹¹ C]CO₂ delivery.

SUBMITTER: Taddei C

PROVIDER: S-EPMC5488231 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature

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Instantaneous Conversion of [11 C]CO2 to [11 C]CO via Fluoride-Activated Disilane Species.

Taddei Carlotta C Bongarzone Salvatore S Gee Antony D AD

Chemistry (Weinheim an der Bergstrasse, Germany) 20170517 32

The development of a fast and novel methodology to generate carbon-11 carbon monoxide ([11 C]CO) from cyclotron-produced carbon-11 carbon dioxide ([11 C]CO2 ) mediated by a fluoride-activated disilane species is described. This methodology allows up to 74 % conversion of [11 C]CO2 to [11 C]CO using commercially available reagents, readily available laboratory equipment and mild reaction conditions (room temperature). As proof of u ...[more]

PMID: 28419627

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Project description:BackgroundThe ?-amyloid radiotracer [11C] PiB is extensively used for the Positron Emission Tomography (PET) diagnosis of Alzheimer's Disease and related dementias. For clinical use, [11C] PiB is produced using the 11C-methylation method ([11C] Methyl iodide or [11C] methyl triflate as 11C-methylation agents), which represents the most employed 11C-labelling strategy for the synthesis of 11C-radiopharmaceuticals. Recently, the use of direct [11C]CO2 fixation for the syntheses of 11C-tracers has gained interest in the radiochemical community due to its importance in terms of radiochemical versatility and for permitting the direct employment of the cyclotron-produced precursor [11C]CO2. This paper presents an optimised alternative one-pot methodology of [11C]CO2 fixation-reduction for the rapid synthesis of [11C] PiB using an automated commercial platform and its quality control.Results[11C] PiB was obtained from a (25.9?±?13.2)% (Average?±?Variation Coefficient, n?=?3) (end of synthesis, decay corrected) radiochemical yield from trapped [11C]CO2 after 1?min of labelling time using PhSiH3 / TBAF as the fixation-reduction system in Diglyme at 150?°C. The radiochemical purity was higher than 95% in all cases, and the molar activity was (61.4?±?1.6) GBq/?mol. The radiochemical yield and activity (EOS) of formulated [11C] PiB from cyclotron-produced [11C]CO2 was (14.8?±?12.1)%, decay corrected) and 9.88?GBq (± 6.0%), respectively. These are higher values compared to that of the 11C-methylation method with [11C]CH3OTf (~?8.3%).ConclusionsThe viability of the system PhSiH3 / TBAF to efficiently promote the radiosynthesis of [11C] PiB via direct [11C]CO2 fixation-reduction has been demonstrated. [11C] PiB was obtained through a fully automated radiosynthesis with a satisfactory yield, purity and molar activity. According to the results, the one-pot methodology employed could reliably yield sufficiently high tracer amounts for preclinical and clinical use.

Dataset Information

Instantaneous Conversion of [¹¹ C]CO₂ to [¹¹ C]CO via Fluoride-Activated Disilane Species.

Publications

Instantaneous Conversion of [<sup>11</sup> C]CO<sub>2</sub> to [<sup>11</sup> C]CO via Fluoride-Activated Disilane Species.

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