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Production of 6-l-[(18)F]Fluoro-m-tyrosine in an Automated Synthesis Module for (11)C-Labeling
6-l-[(18)F]Fluoro-m-tyrosine (6-l-[(18)F]FMT) represents a valuable alternative to 6-l-[(18)F]FDOPA which is conventionally used for the diagnosis and staging of Parkinson’s disease. However, clinical applications of 6-l-[(18)F]FMT have been limited by the paucity of practical production methods for...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8468244/ https://www.ncbi.nlm.nih.gov/pubmed/34577021 http://dx.doi.org/10.3390/molecules26185550 |
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author | Orlovskaya, Viktoriya V. Craig, Austin S. Fedorova, Olga S. Kuznetsova, Olga F. Neumaier, Bernd Krasikova, Raisa N. Zlatopolskiy, Boris D. |
author_facet | Orlovskaya, Viktoriya V. Craig, Austin S. Fedorova, Olga S. Kuznetsova, Olga F. Neumaier, Bernd Krasikova, Raisa N. Zlatopolskiy, Boris D. |
author_sort | Orlovskaya, Viktoriya V. |
collection | PubMed |
description | 6-l-[(18)F]Fluoro-m-tyrosine (6-l-[(18)F]FMT) represents a valuable alternative to 6-l-[(18)F]FDOPA which is conventionally used for the diagnosis and staging of Parkinson’s disease. However, clinical applications of 6-l-[(18)F]FMT have been limited by the paucity of practical production methods for its automated production. Herein we describe the practical preparation of 6-l-[(18)F]FMT using alcohol-enhanced Cu-mediated radiofluorination of Bpin-substituted chiral Ni(II) complex in the presence of non-basic Bu(4)ONTf using a volatile iPrOH/MeCN mixture as reaction solvent. A simple and fast radiolabeling procedure afforded the tracer in 20.0 ± 3.0% activity yield within 70 min. The developed method was directly implemented onto a modified TracerLab FX C Pro platform originally designed for (11)C-labeling. This method enables an uncomplicated switch between (11)C- and (18)F-labeling. The simplicity of the developed procedure enables its easy adaptation to other commercially available remote-controlled synthesis units and paves the way for a widespread application of 6-l-[(18)F]FMT in the clinic. |
format | Online Article Text |
id | pubmed-8468244 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-84682442021-09-27 Production of 6-l-[(18)F]Fluoro-m-tyrosine in an Automated Synthesis Module for (11)C-Labeling Orlovskaya, Viktoriya V. Craig, Austin S. Fedorova, Olga S. Kuznetsova, Olga F. Neumaier, Bernd Krasikova, Raisa N. Zlatopolskiy, Boris D. Molecules Article 6-l-[(18)F]Fluoro-m-tyrosine (6-l-[(18)F]FMT) represents a valuable alternative to 6-l-[(18)F]FDOPA which is conventionally used for the diagnosis and staging of Parkinson’s disease. However, clinical applications of 6-l-[(18)F]FMT have been limited by the paucity of practical production methods for its automated production. Herein we describe the practical preparation of 6-l-[(18)F]FMT using alcohol-enhanced Cu-mediated radiofluorination of Bpin-substituted chiral Ni(II) complex in the presence of non-basic Bu(4)ONTf using a volatile iPrOH/MeCN mixture as reaction solvent. A simple and fast radiolabeling procedure afforded the tracer in 20.0 ± 3.0% activity yield within 70 min. The developed method was directly implemented onto a modified TracerLab FX C Pro platform originally designed for (11)C-labeling. This method enables an uncomplicated switch between (11)C- and (18)F-labeling. The simplicity of the developed procedure enables its easy adaptation to other commercially available remote-controlled synthesis units and paves the way for a widespread application of 6-l-[(18)F]FMT in the clinic. MDPI 2021-09-13 /pmc/articles/PMC8468244/ /pubmed/34577021 http://dx.doi.org/10.3390/molecules26185550 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Orlovskaya, Viktoriya V. Craig, Austin S. Fedorova, Olga S. Kuznetsova, Olga F. Neumaier, Bernd Krasikova, Raisa N. Zlatopolskiy, Boris D. Production of 6-l-[(18)F]Fluoro-m-tyrosine in an Automated Synthesis Module for (11)C-Labeling |
title | Production of 6-l-[(18)F]Fluoro-m-tyrosine in an Automated Synthesis Module for (11)C-Labeling |
title_full | Production of 6-l-[(18)F]Fluoro-m-tyrosine in an Automated Synthesis Module for (11)C-Labeling |
title_fullStr | Production of 6-l-[(18)F]Fluoro-m-tyrosine in an Automated Synthesis Module for (11)C-Labeling |
title_full_unstemmed | Production of 6-l-[(18)F]Fluoro-m-tyrosine in an Automated Synthesis Module for (11)C-Labeling |
title_short | Production of 6-l-[(18)F]Fluoro-m-tyrosine in an Automated Synthesis Module for (11)C-Labeling |
title_sort | production of 6-l-[(18)f]fluoro-m-tyrosine in an automated synthesis module for (11)c-labeling |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8468244/ https://www.ncbi.nlm.nih.gov/pubmed/34577021 http://dx.doi.org/10.3390/molecules26185550 |
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