Cargando…

A Fully Automated Radiosynthesis of [(18)F]Fluoroethyl-Diprenorphine on a Single Module by Use of SPE Cartridges for Preparation of High Quality 2-[(18)F]Fluoroethyl Tosylate

We have developed a new method for automated production of 2-[(18)F]fluoroethyl tosylate ([(18)F]FETos) that enables (18)F-alkylation to provide PET tracers with high chemical purity. The method is based on the removal of excess ethylene glycol bistosylate precursor by precipitation and subsequent f...

Descripción completa

Detalles Bibliográficos
Autores principales: Schoultz, Bent W., Reed, Brian J., Marton, János, Willoch, Frode, Henriksen, Gjermund
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270389/
https://www.ncbi.nlm.nih.gov/pubmed/23787515
http://dx.doi.org/10.3390/molecules18067271
_version_ 1783376687963045888
author Schoultz, Bent W.
Reed, Brian J.
Marton, János
Willoch, Frode
Henriksen, Gjermund
author_facet Schoultz, Bent W.
Reed, Brian J.
Marton, János
Willoch, Frode
Henriksen, Gjermund
author_sort Schoultz, Bent W.
collection PubMed
description We have developed a new method for automated production of 2-[(18)F]fluoroethyl tosylate ([(18)F]FETos) that enables (18)F-alkylation to provide PET tracers with high chemical purity. The method is based on the removal of excess ethylene glycol bistosylate precursor by precipitation and subsequent filtration and purification of the filtrate by means of solid phase extraction cartridges (SPE). The method is integrated to a single synthesis module and thereby provides the advantage over previous methods of not requiring HPLC purification, as demonstrated by the full radiosynthesis of the potent opioid receptor PET tracer [(18)F]fluoroethyldiprenorphine.
format Online
Article
Text
id pubmed-6270389
institution National Center for Biotechnology Information
language English
publishDate 2013
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-62703892018-12-17 A Fully Automated Radiosynthesis of [(18)F]Fluoroethyl-Diprenorphine on a Single Module by Use of SPE Cartridges for Preparation of High Quality 2-[(18)F]Fluoroethyl Tosylate Schoultz, Bent W. Reed, Brian J. Marton, János Willoch, Frode Henriksen, Gjermund Molecules Article We have developed a new method for automated production of 2-[(18)F]fluoroethyl tosylate ([(18)F]FETos) that enables (18)F-alkylation to provide PET tracers with high chemical purity. The method is based on the removal of excess ethylene glycol bistosylate precursor by precipitation and subsequent filtration and purification of the filtrate by means of solid phase extraction cartridges (SPE). The method is integrated to a single synthesis module and thereby provides the advantage over previous methods of not requiring HPLC purification, as demonstrated by the full radiosynthesis of the potent opioid receptor PET tracer [(18)F]fluoroethyldiprenorphine. MDPI 2013-06-20 /pmc/articles/PMC6270389/ /pubmed/23787515 http://dx.doi.org/10.3390/molecules18067271 Text en © 2013 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Schoultz, Bent W.
Reed, Brian J.
Marton, János
Willoch, Frode
Henriksen, Gjermund
A Fully Automated Radiosynthesis of [(18)F]Fluoroethyl-Diprenorphine on a Single Module by Use of SPE Cartridges for Preparation of High Quality 2-[(18)F]Fluoroethyl Tosylate
title A Fully Automated Radiosynthesis of [(18)F]Fluoroethyl-Diprenorphine on a Single Module by Use of SPE Cartridges for Preparation of High Quality 2-[(18)F]Fluoroethyl Tosylate
title_full A Fully Automated Radiosynthesis of [(18)F]Fluoroethyl-Diprenorphine on a Single Module by Use of SPE Cartridges for Preparation of High Quality 2-[(18)F]Fluoroethyl Tosylate
title_fullStr A Fully Automated Radiosynthesis of [(18)F]Fluoroethyl-Diprenorphine on a Single Module by Use of SPE Cartridges for Preparation of High Quality 2-[(18)F]Fluoroethyl Tosylate
title_full_unstemmed A Fully Automated Radiosynthesis of [(18)F]Fluoroethyl-Diprenorphine on a Single Module by Use of SPE Cartridges for Preparation of High Quality 2-[(18)F]Fluoroethyl Tosylate
title_short A Fully Automated Radiosynthesis of [(18)F]Fluoroethyl-Diprenorphine on a Single Module by Use of SPE Cartridges for Preparation of High Quality 2-[(18)F]Fluoroethyl Tosylate
title_sort fully automated radiosynthesis of [(18)f]fluoroethyl-diprenorphine on a single module by use of spe cartridges for preparation of high quality 2-[(18)f]fluoroethyl tosylate
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270389/
https://www.ncbi.nlm.nih.gov/pubmed/23787515
http://dx.doi.org/10.3390/molecules18067271
work_keys_str_mv AT schoultzbentw afullyautomatedradiosynthesisof18ffluoroethyldiprenorphineonasinglemodulebyuseofspecartridgesforpreparationofhighquality218ffluoroethyltosylate
AT reedbrianj afullyautomatedradiosynthesisof18ffluoroethyldiprenorphineonasinglemodulebyuseofspecartridgesforpreparationofhighquality218ffluoroethyltosylate
AT martonjanos afullyautomatedradiosynthesisof18ffluoroethyldiprenorphineonasinglemodulebyuseofspecartridgesforpreparationofhighquality218ffluoroethyltosylate
AT willochfrode afullyautomatedradiosynthesisof18ffluoroethyldiprenorphineonasinglemodulebyuseofspecartridgesforpreparationofhighquality218ffluoroethyltosylate
AT henriksengjermund afullyautomatedradiosynthesisof18ffluoroethyldiprenorphineonasinglemodulebyuseofspecartridgesforpreparationofhighquality218ffluoroethyltosylate
AT schoultzbentw fullyautomatedradiosynthesisof18ffluoroethyldiprenorphineonasinglemodulebyuseofspecartridgesforpreparationofhighquality218ffluoroethyltosylate
AT reedbrianj fullyautomatedradiosynthesisof18ffluoroethyldiprenorphineonasinglemodulebyuseofspecartridgesforpreparationofhighquality218ffluoroethyltosylate
AT martonjanos fullyautomatedradiosynthesisof18ffluoroethyldiprenorphineonasinglemodulebyuseofspecartridgesforpreparationofhighquality218ffluoroethyltosylate
AT willochfrode fullyautomatedradiosynthesisof18ffluoroethyldiprenorphineonasinglemodulebyuseofspecartridgesforpreparationofhighquality218ffluoroethyltosylate
AT henriksengjermund fullyautomatedradiosynthesisof18ffluoroethyldiprenorphineonasinglemodulebyuseofspecartridgesforpreparationofhighquality218ffluoroethyltosylate