One-pot synthesis of high molar activity 6-[18F]fluoro-l-DOPA by Cu-mediated fluorination of a BPin precursor
Journal Article
·
· Organic and Biomolecular Chemistry
- Univ. of Michigan, Ann Arbor, MI (United States). Dept. of Radiology
- Univ. of Michigan, Ann Arbor, MI (United States). Dept. of Radiology. Dept. of Medicinal Chemistry
- Univ. of Michigan, Ann Arbor, MI (United States). Dept. of Chemistry
- AbbVie Translational Imaging, North Chicago, IL (United States)
A one-pot two-step synthesis of 6-[18F]fluoro-L-DOPA ([18F]FDOPA) has been developed involving Cu-mediated radiofluorination of a pinacol boronate ester precursor. The method is fully automated, provides [18F]FDOPA in good activity yield (104 ± 16 mCi, 6 ± 1%), excellent radiochemical purity (>99%) and high molar activity (3799 ± 2087 Ci mmol-1), n = 3, and has been validated to produce the radiotracer for human use.
- Research Organization:
- Univ. of Michigan, Ann Arbor, MI (United States)
- Sponsoring Organization:
- USDOE Office of Science (SC), Basic Energy Sciences (BES)
- Grant/Contract Number:
- SC0012484
- OSTI ID:
- 1802363
- Alternate ID(s):
- OSTI ID: 1562735
- Journal Information:
- Organic and Biomolecular Chemistry, Vol. 17, Issue 38; ISSN 1477-0520
- Publisher:
- Royal Society of ChemistryCopyright Statement
- Country of Publication:
- United States
- Language:
- English
Cited by: 23 works
Citation information provided by
Web of Science
Web of Science
Hot off the Press
|
journal | January 2019 |
Late-Stage Copper-Catalyzed Radiofluorination of an Arylboronic Ester Derivative of Atorvastatin
|
journal | November 2019 |
Approaches to PET Imaging of Glioblastoma
|
journal | January 2020 |
Similar Records
High yield synthesis of 6-(/sup 18/F)fluoro-L-dopa by regioselective fluorination of protected L-dopa with (/sup 18/F)acetylhypofluorite
Synthesis of N-formyl-3,4-di-t-butoxycarbonyloxy-6(trimethylstannyl)-L-phenylalanine ethyl ester and its regioselective radiofluorodestannylation to 6-[{sup 18}F]fluoro-L-dopa
Synthesis of N-formyl-3,4-di-t-butoxycarbonyloxy-6-(trimethylstannyl)-L-phenylalanine ethyl ester and its regioselective radiofluorodestannylation to 6-[.sup.18 F]fluoro-L-dopa
Journal Article
·
Mon Dec 01 00:00:00 EST 1986
· J. Nucl. Med.; (United States)
·
OSTI ID:1802363
Synthesis of N-formyl-3,4-di-t-butoxycarbonyloxy-6(trimethylstannyl)-L-phenylalanine ethyl ester and its regioselective radiofluorodestannylation to 6-[{sup 18}F]fluoro-L-dopa
Patent
·
Tue Feb 28 00:00:00 EST 1995
·
OSTI ID:1802363
+1 more
Synthesis of N-formyl-3,4-di-t-butoxycarbonyloxy-6-(trimethylstannyl)-L-phenylalanine ethyl ester and its regioselective radiofluorodestannylation to 6-[.sup.18 F]fluoro-L-dopa
Patent
·
Sun Jan 01 00:00:00 EST 1995
·
OSTI ID:1802363
+1 more