Reactive Palladium–Ligand Complexes for 11C-Carbonylation at Ambient Pressure: A Breakthrough in Carbon-11 Chemistry

Author:

Dahl Kenneth12,Lindberg Anton3,Vasdev Neil34ORCID,Schou Magnus12

Affiliation:

1. PET Science Centre, Precision Medicine and Biosamples, Oncology R&D, AstraZeneca, Karolinska Institutet, SE-17176 Stockholm, Sweden

2. Department of Clinical Neuroscience, Centre for Psychiatry Research, Karolinska Institutet and Stockholm County Council, SE-17176 Stockholm, Sweden

3. Azrieli Centre for Neuro-Radiochemistry, Brain Health Imaging Centre, Centre for Addiction and Mental Health, 250 College St., Toronto, ON M5T1R8, Canada

4. Department of Psychiatry, University of Toronto, 250 College St., Toronto, ON M5T1R8, Canada

Abstract

The Pd–Xantphos-mediated 11C-carbonylation protocol (also known as the “Xantphos- method”), due to its simplistic and convenient nature, has facilitated researchers in meeting a longstanding need for preparing 11C-carbonyl-labeled radiopharmaceuticals at ambient pressure for positron emission tomography (PET) imaging and drug discovery. This development could be viewed as a breakthrough in carbon-11 chemistry, as evidenced by the rapid global adoption of the method by the pharmaceutical industry and academic laboratories worldwide. The method has been fully automated for the good manufacturing practice (GMP)-compliant production of novel radiopharmaceuticals for human use, and it has been adapted for “in-loop” reactions and microwave technology; an impressive number of 11C-labeled compounds (>100) have been synthesized. Given the simplicity and efficiency of the method, as well as the abundance of carbonyl groups in bioactive drug molecules, we expect that this methodology will be even more widely adopted in future PET radiopharmaceutical research and drug development.

Publisher

MDPI AG

Subject

Drug Discovery,Pharmaceutical Science,Molecular Medicine

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