PERFLUORO-ARYLIODONIUM SALTS IN NUCLEOPHILIC AROMATIC 18F-FLUORINATION

摘要

The present invention describes using fluorous chemistry in n.c.a. nucleophilic aromatic 18F-fluorination reactions by using perfluoro-aryliodonium salts as a precursor for aromatic nucleophilic substitution using a [18F] F-anion to displace a suitable leaving group from an electron deficient benzene ring. The results showed that using perfluoro-aryliodonium salts as a precursor is a suitable leaving group for n. c. a. nucleophilic aromatic 18F-fluorination in synthesis. The PT-precursor seems to be quite stable. In an attempt to purify the crude 18F-labeled product using fluorous solid phase extraction (F-SPE), the radio labeled impurities decreased significantly. Thus, it is possible to use this PT methodology to simplify and speed up purification methods.