PET Chemistry: The Driving Force in Molecular Imaging

Description

Personalized medicine employing patient-based tailor-made therapeutic drugs is taking over treatment paradigms in a variety of ?elds in oncology and the central nervous system. The success of such therapies is mainly dependent on ef?cacious therapeutic drugs and a selective imaging probe for identi?cation of potential responders as well as therapy monitoring for an early bene?t assessment. Molecular imaging (MI) is based on the selective and speci?c interaction of a molecular probe with a biological target which is visualized through nuclear, magnetic resonance, near infrared or other methods. Therefore it is the method of choice for patient selection and therapy monitoring as well as for speci?c e- point monitoring in modern drug development. PET (positron emitting tomography), a nuclear medical imaging modality, is ideally suited to produce three-dimensional images of various targets or processes. The rapidly increasing demand for highly selective probes for MI strongly pushes the development of new PET tracers and PET chemistry. ‘PET chemistry’ can be de?ned as the study of positron-emitting compounds regarding their synthesis, structure, composition, reactivity, nuclear properties and processes and their properties in natural and - natural environments. In practice PET chemistry is strongly in?uenced by the unique properties of the radioisotopes used (e. g. , half-life, che- cal reactivity, etc. ) and integrates scienti?c aspects of nuclear-, organic-, inorganic- and biochemistry. Front Matter....Pages I-XII Molecular Imaging with PET — Open Questions?....Pages 1-13 Fluorine-18 Labeling Methods: Features and Possibilities of Basic Reactions....Pages 15-50 Fluorine-18 Labeling of Small Molecules: The Use of 18 F-Labeled Aryl Fluorides Derived from No-Carrier-Added [ 18 F]Fluoride as Labeling Precursors....Pages 51-78 Fluorine-18 Labeling of Peptides and Proteins....Pages 79-111 [ 18 F]Fluoropyridines: From Conventional Radiotracers to the Labeling of Macromolecules Such as Proteins and Oligonucleotides....Pages 113-157 Production of Non-standard PET Radionuclides and the Application of Radiopharmaceuticals Labeled with these Nuclides....Pages 159-181 Carbon-11 Labeling Chemistry Based upon [ 11 C]Methyl Iodide....Pages 183-213 68 Ga-PET Radiopharmacy: A Generator-Based Alternative to 18 F-Radiopharmacy....Pages 215-242 Microwaving in F-18 Chemistry: Quirks and Tweaks....Pages 243-269 Micro-reactors for PET Tracer Labeling....Pages 271-287 Synthesis Modules and Automation in F-18 Labeling....Pages 289-316 Pharmacological Prerequisites for PET Ligands and Practical Issues in Preclinical PET Research....Pages 317-327 Positron Emission Tomography Imaging as a Key Enabling Technology in Drug Development....Pages 329-339 Back Matter....Pages 341-345