Automated Synthesis of PET Radiotracers by Copper-mediated 18F-Fluorination of Organoborons: Importance of the Order of Addition and Competing Protodeborylation
| Autor: | Naoko Ichiishi, Andrew V. Mossine, Justin J. Bailey, Vadim Bernard-Gauthier, Peter Scott, Ralf Schirrmacher, Allen F. Brooks, Melanie S. Sanford |
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| Jazyk: | angličtina |
| Rok vydání: | 2018 |
| Předmět: |
Fluorine Radioisotopes
Pet chemistry Copper mediated 010402 general chemistry Ligands 01 natural sciences Biochemistry Article Analytical Chemistry Automation Drug Discovery medicine Receptor trkB Radiology Nuclear Medicine and imaging Receptor trkC Spectroscopy Boron medicine.diagnostic_test 010405 organic chemistry Chemistry Organic Chemistry Radiochemistry Imidazoles Automated radiosynthesis 0104 chemical sciences Pyridazines High specific activity Positron emission tomography Yield (chemistry) Positron-Emission Tomography Radiopharmaceuticals Copper |
| Popis: | In this paper, we describe the use of Cu-mediated [18 F]fluorodeboronation for the automated production of positron emission tomography radiotracers suitable for clinical use. Two recurrent issues with the method, low radiochemical conversion on automation and protoarene byproduct purification issues, have been successfully addressed. The new method was utilized to produce sterile injectable doses of [18 F]-(±)-IPMICF17, a positron emission tomography radiotracer for tropomyosin receptor kinase B/C, using an automated synthesis module. The product was isolated in 1.9 ± 0.1% isolated radiochemical yield, excellent radiochemical purity (>99%), and high specific activity (5294 ± 1227 Ci/mmol). Quality control testing confirmed that doses were suitable for clinical use. |
| Databáze: | OpenAIRE |
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