(F-18)N-fluoro-N-alkylsulfonamides: Novel reagents for radiofluorination

Conference · Sun Jan 01 04:00:00 EST 1984 · J. Nucl. Med.; (United States)

OSTI ID:6575443

Satyamurthy, N; Bida, G T; Barrio, J R; Phelps, M E

The authors report here a new regioselective method for radiofluorination which involves the use of organometallic compounds as substrates. (F-18)N-Fluoro-N-alkylsulfonamides, prepared by fluorination of N-alkysulfonamides with (F-18) fluorine, react readily with aryllithium or arylGrignard reagents to give (F-18)fluoraryl derivatives. As a typical example, (F-18)fluorine gas (50 micromol) diluted in neon (0.2%, v/v/) prepared using the Ne-20 (d, ..cap alpha..) nuclear reaction, is reacted with N-endo-norbornyl (p-tolyl)suflonamide at room temperature and the product, (F-18)N-fluoro-N-endo-norborny(p-tolyl)sulfonamide, is then treated with phenyllithium or phenylmagnesium bromide to produce (F-18)fluorobenzene in 60-70% radiochemical fields. This reaction represents a novel, general route to (F-18)arylfluorides of moderate specific activity (1-10 Ci/mmole), and is potentially valuable for the synthesis of a variety of radiotracers, including radiolabeled enzyme inhibitors and neurotransmitter ligands for application in positron emission tomography.

• Research Organization: UCLA School of Medicine, Los Angeles, CA
• OSTI ID: 6575443
• Report Number(s): CONF-840619-
• Conference Information: Journal Name: J. Nucl. Med.; (United States) Journal Volume: 25:5
• Country of Publication: United States
• Language: English

Related Subjects

38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
400702 -- Radiochemistry & Nuclear Chemistry-- Properties of Radioactive Materials
550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
ALKYLATED AROMATICS
AMIDES
ANTI-INFECTIVE AGENTS
ANTIMICROBIAL AGENTS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
CHEMICAL PREPARATION
CHEMICAL REACTION KINETICS
CHEMICAL REACTION YIELD
CHEMICAL REACTIONS
CHEMISTRY
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
DRUGS
EMISSION COMPUTED TOMOGRAPHY
ENZYME INHIBITORS
FLUORINATION
FLUORINE 18
FLUORINE ISOTOPES
HALOGENATION
HOURS LIVING RADIOISOTOPES
ISOTOPES
KINETICS
LABELLED COMPOUNDS
LABELLING
LIGANDS
LIGHT NUCLEI
NEUROREGULATORS
NUCLEI
ODD-ODD NUCLEI
ORGANIC COMPOUNDS
ORGANIC FLUORINE COMPOUNDS
ORGANIC HALOGEN COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANIC SULFUR COMPOUNDS
POSITRON COMPUTED TOMOGRAPHY
RADIOCHEMISTRY
RADIOISOTOPES
RADIOPHARMACEUTICALS
REACTION KINETICS
REAGENTS
SULFONAMIDES
SYNTHESIS
TOMOGRAPHY
YIELDS