Fluorine-18 labeling methods: Features and possibilities of basic reactions

Abstract

Many experimental and established tracers make fluorine- 18 the most widely used radionuclide in positron emission tomography with an increasing demand for new or simpler 18F-labeling procedures. After a brief summary of the advantages of the nuclide and its major production routes, the basic features of the principal radiofluorination methods are described. These comprise direct electrophilic and nucleophilic processes, or in case of more complex molecules, the labeling of synthons and prosthetic groups for indirect built-up syntheses. While addressing the progress of no-carrier-added 18F-labeling procedures, the following chapters on more specific topics in this book are introduced. Emphasis is given to radiofluorination of arenes--especially with iodonium leaving groups. Examples of radiopharmaceutical syntheses are mentioned in order to illustrate strategic concepts of labeling with fluorine-18.