Automated production of 11C‐labeled carboxylic acids and esters via “in‐loop” 11C‐carbonylation using GE FX synthesis modules
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Published:2023-08-22
Issue:
Volume:
Page:
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ISSN:0362-4803
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Container-title:Journal of Labelled Compounds and Radiopharmaceuticals
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language:en
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Short-container-title:Labelled Comp Radiopharmac
Author:
Kaur Tanpreet1ORCID,
Wright Jay S.1ORCID,
Henderson Bradford D.1,
Godinez Jonathan2,
Shao Xia1ORCID,
Scott Peter J. H.12ORCID
Affiliation:
1. Division of Nuclear Medicine, Department of Radiology University of Michigan Medical School Ann Arbor Michigan USA
2. Interdepartmental Program in Medicinal Chemistry University of Michigan Ann Arbor Michigan USA
Abstract
An in‐loop 11C‐carbonylation process for the radiosynthesis of 11C‐carboxylic acids and esters from halide precursors has been developed. The reaction proceeds at room temperature under mild conditions and enables 11C‐carbonylation of both electron deficient and electron rich (hetero)aromatic halides to provide 11C‐carboxylic acids and esters in good to excellent radiochemical yields, high radiochemical purity, and excellent molar activity. The process has been fully automated using commercial radiochemistry synthesis modules, and application to clinical production is demonstrated via validated cGMP radiosyntheses of [11C]bexarotene and [11C]acetoacetic acid.
Funder
National Institute of Biomedical Imaging and Bioengineering
Subject
Organic Chemistry,Spectroscopy,Drug Discovery,Radiology, Nuclear Medicine and imaging,Biochemistry,Analytical Chemistry
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