Radiosynthesis of the diastereomerically pure (E)-[11 C]ABP688

Hussein Bdair; I-Huang Tsai; Kelly Smart; Chawki Benkelfat; Marco Leyton; Alexey Kostikov

doi:10.1002/jlcr.3802

Radiosynthesis of the diastereomerically pure (E)-[¹¹ C]ABP688

J Labelled Comp Radiopharm. 2019 Oct;62(12):860-864. doi: 10.1002/jlcr.3802. Epub 2019 Sep 18.

Authors

Hussein Bdair^{1

2}, I-Huang Tsai³, Kelly Smart⁴, Chawki Benkelfat², Marco Leyton², Alexey Kostikov^{1

3

5}

Affiliations

¹ McGill University, Montreal Neurological Institute, Montreal, Quebec, Canada.
² McGill University, Department of Psychiatry, Montreal, Quebec, Canada.
³ McGill University, McConnell Brain Imaging Centre, Montreal Neurological Institute, Montreal, Quebec, Canada.
⁴ Yale University School of Medicine, Yale PET Center, New Haven, Connecticut.
⁵ Department of Neurology and Neurosurgery, McGill University, Montreal, Quebec, Canada.

PMID: 31418468
DOI: 10.1002/jlcr.3802

Abstract

We report an efficient protocol for the radiosynthesis of diastereomerically pure (E)-[¹¹ C]ABP688, a positron emission tomography (PET) tracer for metabotropic glutamate type 5 (mGlu5) receptor imaging. The protocol reliably provides sterile and pyrogen-free formulation of (E)-[¹¹ C]ABP688 suitable for preclinical and clinical PET imaging with >99% diastereomeric excess (d.e.), >99% overall radiochemical purity (RCP), 14.9 ± 4.3% decay-corrected radiochemical yield (RCY), and 148.86 ± 79.8 GBq/μmol molar activity in 40 minutes from the end of bombardment.

Keywords: (E)-[11C]ABP688; PET tracers; mGlu5 receptors; radiosynthesis.

MeSH terms

Carbon Radioisotopes / chemistry*
Chemistry Techniques, Synthetic
Oximes / chemical synthesis*
Oximes / chemistry*
Positron-Emission Tomography
Pyridines / chemical synthesis*
Pyridines / chemistry*
Radiochemistry
Stereoisomerism

Substances

3-(6-methylpyridin-2-ylethynyl)cyclohex-2-enone-O-methyloxime
Carbon Radioisotopes
Carbon-11
Oximes
Pyridines