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Title: Synthesis of fluorinated radiopharmaceuticals via electrochemical fluorination

Abstract

Provided herein are methods and compositions for the electrochemical selective radiofluorination of aromatic molecules. The resulting fluorine-18 labeled compounds are ideal radionuclides for use in Positron Emission Tomography (PET); they are also difficult to radiolabel efficiently and with high specific activity using existing approaches. For example, radiopharmaceuticals such as [F18]L-DOPA, which is indispensable in PET brain disease imaging, may be made electrochemically with high radiochemical yield and high specific activity using 18F-. The invention process described herein opens new possibilities and provides wider access to PET tracers such as 18F-L-Dopa, since 18F- is much more widely available than the 18F2, currently used for synthesis of electron rich substrates.

Inventors:
; ;
Issue Date:
Research Org.:
Univ. of California, Oakland, CA (United States)
Sponsoring Org.:
USDOE
OSTI Identifier:
1637790
Patent Number(s):
10597340
Application Number:
14/937,649
Assignee:
The Regents of the University of California (Oakland, CA)
Patent Classifications (CPCs):
C - CHEMISTRY C07 - ORGANIC CHEMISTRY C07C - ACYCLIC OR CARBOCYCLIC COMPOUNDS
C - CHEMISTRY C07 - ORGANIC CHEMISTRY C07B - GENERAL METHODS OF ORGANIC CHEMISTRY
Resource Type:
Patent
Resource Relation:
Patent File Date: 11/10/2015
Country of Publication:
United States
Language:
English

Citation Formats

Sadeghi, Saman, He, Qinggang, and Lebedev, Artem. Synthesis of fluorinated radiopharmaceuticals via electrochemical fluorination. United States: N. p., 2020. Web.
Sadeghi, Saman, He, Qinggang, & Lebedev, Artem. Synthesis of fluorinated radiopharmaceuticals via electrochemical fluorination. United States.
Sadeghi, Saman, He, Qinggang, and Lebedev, Artem. Tue . "Synthesis of fluorinated radiopharmaceuticals via electrochemical fluorination". United States. https://www.osti.gov/servlets/purl/1637790.
@article{osti_1637790,
title = {Synthesis of fluorinated radiopharmaceuticals via electrochemical fluorination},
author = {Sadeghi, Saman and He, Qinggang and Lebedev, Artem},
abstractNote = {Provided herein are methods and compositions for the electrochemical selective radiofluorination of aromatic molecules. The resulting fluorine-18 labeled compounds are ideal radionuclides for use in Positron Emission Tomography (PET); they are also difficult to radiolabel efficiently and with high specific activity using existing approaches. For example, radiopharmaceuticals such as [F18]L-DOPA, which is indispensable in PET brain disease imaging, may be made electrochemically with high radiochemical yield and high specific activity using 18F-. The invention process described herein opens new possibilities and provides wider access to PET tracers such as 18F-L-Dopa, since 18F- is much more widely available than the 18F2, currently used for synthesis of electron rich substrates.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {2020},
month = {3}
}

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