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Automated Synthesis of (18)F-BCPP-EF {2-tert-Butyl-4-Chloro-5-{6-[2-(2[(18)F]fluoroethoxy)-Ethoxy]-Pyridin-3-ylmethoxy}-2H-Pyridazin-3-One for Imaging of Mitochondrial Complex 1 in Parkinson’s Disease

Mitochondrial complex I (MC-I) is an essential component of brain bioenergetics and can be quantified and studied using positron emission tomography (PET). A specific high affinity (18)F radiotracer for MC-I enables monitoring of neurodegenerative disease progression and pathology via PET imaging. T...

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Autores principales: Kaur, Tanpreet, Brooks, Allen F., Liddell, Katherine M., Henderson, Bradford D., Hockley, Brian G., Bohnen, Nicolaas I., Albin, Roger L., Scott, Peter J. H.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9005973/
https://www.ncbi.nlm.nih.gov/pubmed/35433631
http://dx.doi.org/10.3389/fchem.2022.878835
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author Kaur, Tanpreet
Brooks, Allen F.
Liddell, Katherine M.
Henderson, Bradford D.
Hockley, Brian G.
Bohnen, Nicolaas I.
Albin, Roger L.
Scott, Peter J. H.
author_facet Kaur, Tanpreet
Brooks, Allen F.
Liddell, Katherine M.
Henderson, Bradford D.
Hockley, Brian G.
Bohnen, Nicolaas I.
Albin, Roger L.
Scott, Peter J. H.
author_sort Kaur, Tanpreet
collection PubMed
description Mitochondrial complex I (MC-I) is an essential component of brain bioenergetics and can be quantified and studied using positron emission tomography (PET). A specific high affinity (18)F radiotracer for MC-I enables monitoring of neurodegenerative disease progression and pathology via PET imaging. To facilitate clinical research studies tracking MC-I activity in Parkinson’s disease and other neurodegenerative diseases, a fully automated synthesis of the recently described 2-tert-butyl-4-chloro-5-{6-[2-(2[(18)F]fluoroethoxy)-ethoxy]-pyridin-3-ylmethoxy}-2H-pyridazin-3-one ([(18)F] BCPP-EF, [ ( 18 ) F]1) was developed. We report the first automated synthesis [(18)F]BCPP-EF using a green radiochemistry approach. The radiotracer was synthesized with good radiochemical yield, excellent radiochemical purity, and high molar activity.
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spelling pubmed-90059732022-04-14 Automated Synthesis of (18)F-BCPP-EF {2-tert-Butyl-4-Chloro-5-{6-[2-(2[(18)F]fluoroethoxy)-Ethoxy]-Pyridin-3-ylmethoxy}-2H-Pyridazin-3-One for Imaging of Mitochondrial Complex 1 in Parkinson’s Disease Kaur, Tanpreet Brooks, Allen F. Liddell, Katherine M. Henderson, Bradford D. Hockley, Brian G. Bohnen, Nicolaas I. Albin, Roger L. Scott, Peter J. H. Front Chem Chemistry Mitochondrial complex I (MC-I) is an essential component of brain bioenergetics and can be quantified and studied using positron emission tomography (PET). A specific high affinity (18)F radiotracer for MC-I enables monitoring of neurodegenerative disease progression and pathology via PET imaging. To facilitate clinical research studies tracking MC-I activity in Parkinson’s disease and other neurodegenerative diseases, a fully automated synthesis of the recently described 2-tert-butyl-4-chloro-5-{6-[2-(2[(18)F]fluoroethoxy)-ethoxy]-pyridin-3-ylmethoxy}-2H-pyridazin-3-one ([(18)F] BCPP-EF, [ ( 18 ) F]1) was developed. We report the first automated synthesis [(18)F]BCPP-EF using a green radiochemistry approach. The radiotracer was synthesized with good radiochemical yield, excellent radiochemical purity, and high molar activity. Frontiers Media S.A. 2022-03-30 /pmc/articles/PMC9005973/ /pubmed/35433631 http://dx.doi.org/10.3389/fchem.2022.878835 Text en Copyright © 2022 Kaur, Brooks, Liddell, Henderson, Hockley, Bohnen, Albin and Scott. https://creativecommons.org/licenses/by/4.0/This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Chemistry
Kaur, Tanpreet
Brooks, Allen F.
Liddell, Katherine M.
Henderson, Bradford D.
Hockley, Brian G.
Bohnen, Nicolaas I.
Albin, Roger L.
Scott, Peter J. H.
Automated Synthesis of (18)F-BCPP-EF {2-tert-Butyl-4-Chloro-5-{6-[2-(2[(18)F]fluoroethoxy)-Ethoxy]-Pyridin-3-ylmethoxy}-2H-Pyridazin-3-One for Imaging of Mitochondrial Complex 1 in Parkinson’s Disease
title Automated Synthesis of (18)F-BCPP-EF {2-tert-Butyl-4-Chloro-5-{6-[2-(2[(18)F]fluoroethoxy)-Ethoxy]-Pyridin-3-ylmethoxy}-2H-Pyridazin-3-One for Imaging of Mitochondrial Complex 1 in Parkinson’s Disease
title_full Automated Synthesis of (18)F-BCPP-EF {2-tert-Butyl-4-Chloro-5-{6-[2-(2[(18)F]fluoroethoxy)-Ethoxy]-Pyridin-3-ylmethoxy}-2H-Pyridazin-3-One for Imaging of Mitochondrial Complex 1 in Parkinson’s Disease
title_fullStr Automated Synthesis of (18)F-BCPP-EF {2-tert-Butyl-4-Chloro-5-{6-[2-(2[(18)F]fluoroethoxy)-Ethoxy]-Pyridin-3-ylmethoxy}-2H-Pyridazin-3-One for Imaging of Mitochondrial Complex 1 in Parkinson’s Disease
title_full_unstemmed Automated Synthesis of (18)F-BCPP-EF {2-tert-Butyl-4-Chloro-5-{6-[2-(2[(18)F]fluoroethoxy)-Ethoxy]-Pyridin-3-ylmethoxy}-2H-Pyridazin-3-One for Imaging of Mitochondrial Complex 1 in Parkinson’s Disease
title_short Automated Synthesis of (18)F-BCPP-EF {2-tert-Butyl-4-Chloro-5-{6-[2-(2[(18)F]fluoroethoxy)-Ethoxy]-Pyridin-3-ylmethoxy}-2H-Pyridazin-3-One for Imaging of Mitochondrial Complex 1 in Parkinson’s Disease
title_sort automated synthesis of (18)f-bcpp-ef {2-tert-butyl-4-chloro-5-{6-[2-(2[(18)f]fluoroethoxy)-ethoxy]-pyridin-3-ylmethoxy}-2h-pyridazin-3-one for imaging of mitochondrial complex 1 in parkinson’s disease
topic Chemistry
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9005973/
https://www.ncbi.nlm.nih.gov/pubmed/35433631
http://dx.doi.org/10.3389/fchem.2022.878835
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