Background
The β-amyloid radiotracer [
11
C] PiB is extensively used for the Positron Emission Tomography (PET) diagnosis of Alzheimer’s Disease and related dementias. For clinical use, [
11
C] PiB is produced using the
11
C-methylation method ([
11
C] Methyl iodide or [
11
C] methyl triflate as
11
C-methylation agents), which represents the most employed
11
C-labelling strategy for the synthesis of
11
C-radiopharmaceuticals. Recently, the use of direct [
11
C]CO
2
fixation for the syntheses of
11
C-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 [
11
C]CO
2
.
This paper presents an optimised alternative one-pot methodology of [
11
C]CO
2
fixation-reduction for the rapid synthesis of [
11
C] PiB using an automated commercial platform and its quality control.
Results
[
11
C] PiB was obtained from a (25.9 ± 13.2)% (Average ± Variation Coefficient,
n
= 3) (end of synthesis, decay corrected) radiochemical yield from trapped [
11
C]CO
2
after 1 min of labelling time using PhSiH
3
/ 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/μmol. The radiochemical yield and activity (EOS) of formulated [
11
C] PiB from cyclotron-produced [
11
C]CO
2
was (14.8 ± 12.1)%, decay corrected) and 9.88 GBq (± 6.0%), respectively. These are higher values compared to that of the
11
C-methylation method with [
11
C]CH
3
OTf (~ 8.3%).
Conclusions
The viability of the system PhSiH
3
/ TBAF to efficiently promote the radiosynthesis of [
11
C] PiB via direct [
11
C]CO
2
fixation-reduction has been demonstrated. [
11
C] 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.
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