The development of a simple process for producing medicinal diagnostic 18F agents for molecular imaging using positron-emission-tomography
A range of resin bound sulfonate ester linkers were developed for use in the resin-linker-vector (RLV) approach for the synthesis of [18F]-fluoride radiotracers for use as imaging agents in positron-emission-tomography (PET). The RLV strategy immobilises a precursor to the desired radiotracer on a s...
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University of Southampton
2010
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ndltd-bl.uk-oai-ethos.bl.uk-5235512018-09-05T03:21:06ZThe development of a simple process for producing medicinal diagnostic 18F agents for molecular imaging using positron-emission-tomographyTopley, Amy ClareBrown, Richard2010A range of resin bound sulfonate ester linkers were developed for use in the resin-linker-vector (RLV) approach for the synthesis of [18F]-fluoride radiotracers for use as imaging agents in positron-emission-tomography (PET). The RLV strategy immobilises a precursor to the desired radiotracer on a solid support which is cleaved on exposure to [18F]-fluoride ion to give the 18F-labelled radiotracer in solution. The RLV methodology allows for easier purification of the 18F-labelled radiotracer as a simple filtration step removes the unreacted starting material and the cleaved resin. Synthetic routes to a 4-allkylphenylsulfonate linker and a 4-nitrophenylsulfonate linker were developed and these were shown to work as desired as part of the RLV construct in [19F]-fluoridolysis reactions. [18F]-Fluoridolysis reactions using the 4-alkylphenylsulfonate linker gave the desired 18F-labelled product in excellent radiochemical purity. The RLV strategy with this linker type was applied in a new synthetic route to O-(2-[18F]-fluoroethyl)-L-tyrosine. A fluorinated analogue of Alzheimer’s disease drug (−)-galanthamine was synthesised with complete stereocontrol as a potential new imaging agent for use in PET.547.02QD ChemistryUniversity of Southamptonhttps://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.523551https://eprints.soton.ac.uk/167749/Electronic Thesis or Dissertation |
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547.02 QD Chemistry |
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547.02 QD Chemistry Topley, Amy Clare The development of a simple process for producing medicinal diagnostic 18F agents for molecular imaging using positron-emission-tomography |
description |
A range of resin bound sulfonate ester linkers were developed for use in the resin-linker-vector (RLV) approach for the synthesis of [18F]-fluoride radiotracers for use as imaging agents in positron-emission-tomography (PET). The RLV strategy immobilises a precursor to the desired radiotracer on a solid support which is cleaved on exposure to [18F]-fluoride ion to give the 18F-labelled radiotracer in solution. The RLV methodology allows for easier purification of the 18F-labelled radiotracer as a simple filtration step removes the unreacted starting material and the cleaved resin. Synthetic routes to a 4-allkylphenylsulfonate linker and a 4-nitrophenylsulfonate linker were developed and these were shown to work as desired as part of the RLV construct in [19F]-fluoridolysis reactions. [18F]-Fluoridolysis reactions using the 4-alkylphenylsulfonate linker gave the desired 18F-labelled product in excellent radiochemical purity. The RLV strategy with this linker type was applied in a new synthetic route to O-(2-[18F]-fluoroethyl)-L-tyrosine. A fluorinated analogue of Alzheimer’s disease drug (−)-galanthamine was synthesised with complete stereocontrol as a potential new imaging agent for use in PET. |
author2 |
Brown, Richard |
author_facet |
Brown, Richard Topley, Amy Clare |
author |
Topley, Amy Clare |
author_sort |
Topley, Amy Clare |
title |
The development of a simple process for producing medicinal diagnostic 18F agents for molecular imaging using positron-emission-tomography |
title_short |
The development of a simple process for producing medicinal diagnostic 18F agents for molecular imaging using positron-emission-tomography |
title_full |
The development of a simple process for producing medicinal diagnostic 18F agents for molecular imaging using positron-emission-tomography |
title_fullStr |
The development of a simple process for producing medicinal diagnostic 18F agents for molecular imaging using positron-emission-tomography |
title_full_unstemmed |
The development of a simple process for producing medicinal diagnostic 18F agents for molecular imaging using positron-emission-tomography |
title_sort |
development of a simple process for producing medicinal diagnostic 18f agents for molecular imaging using positron-emission-tomography |
publisher |
University of Southampton |
publishDate |
2010 |
url |
https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.523551 |
work_keys_str_mv |
AT topleyamyclare thedevelopmentofasimpleprocessforproducingmedicinaldiagnostic18fagentsformolecularimagingusingpositronemissiontomography AT topleyamyclare developmentofasimpleprocessforproducingmedicinaldiagnostic18fagentsformolecularimagingusingpositronemissiontomography |
_version_ |
1718728645358387200 |