Nucl Med Mol Imaging.  2009 Feb;43(1):1-9.

A Novel Aromatic Fluorine-18 Labeling Method Using Iodonium Salts Precursor

• Moon BS
• Lee BC
• Kim SE

Abstract

As many new drug substances contained various aromatic rings and fluorine attached to an electron rich aromatic ring or on the meta-position, a strategy towards improvement in aromatic fluorination of these compounds is highly desirable. The introduction of fluorine-18 onto aromatic rings showed in the limited condition containing electron withdrawing group (EWG) on the para- or ortho-position to get reasonable radiochemical yield so far. No-carrier added (NCA) [18F]fluoroarene syntheses by iodonium salts recently reported that has the potential to greatly increase the yield in systems or positions that normally not reactive enough to give sufficient yields in simple model reaction. This review describes the methodological approach towards effective aromatic fluorination by diaryliodonium salts and future prospects in an application of novel PET radiotracer.

Keyword

Aromatic fluorination; fluorine-18; diaryliodonium salts; PET

MeSH Terms

Electrons
Fluorine
Halogenation
Salts
Fluorine
Salts