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In recent years, organo-fluorine chemistry has made a marked impact on the design and synthesis of a large variety of biologically active molecules, such as steroids, carbohydrates, amines, amino acids, peptides and other natural products. Naturally occurring amino acids play a pivotal role in living systems, and therefore synthetic fluorine-containing amino acids have been of significant interest to researchers working towards the understanding and modification of physiological processes. Fluorine-containing Amino Acids: is the first volume devoted to the synthesis and properties of fluorine-containing amino acids pays special attention to the preparation of enantiomerically pure acids (which are essential to the modern pharmaceutical industry) deals with a rapidly expanding field of research has been written by experienced researchers who are responsible for many developments in the field highlights the interdisciplinary nature of this topic Fluorine-containing Amino Acids is the only dedicated reference in this subject and will be essential for researchers in synthetic organic, peptide, natural product, and medicinal chemistry and biochemistry.
Fluorine Chemistry, Volume IV provides an extensive survey and discussion on the physiological properties of fluoride ion and substances capable of producing it in aqueous solution. This book elaborates the detrimental effects of excessive fluoride ingestion, through the beneficial effects of optimal amounts, to recognized detrimental effects, such as dental caries accompanied by suboptimal fluoride intake. Fluoride metabolism is discussed in detail, including the capacity for storage of fluoride by the bones and rates of excretion of fluoride from the body. This text also covers the relation of fluoride ion to the health of teeth and bones. This publication is a good source for chemists and clinicians intending to acquire knowledge of the biological effects of fluoride.
The extraordinary potential of fluorine-containing molecules in medicinal chemistry and chemical biology has been recognized by researchers outside of the traditional fluorine chemistry field, and thus a new wave of fluorine chemistry is rapidly expanding its biomedical frontiers. With several of the best selling drugs in the world crucially containing fluorine atoms, the incorporation of fluorine to drug leads has become an essential practice in biomedical research, especially for drug design and discovery as well as development. Focusing on the unique and significant roles that fluorine plays in medicinal chemistry and chemical biology, this book reviews recent advances and future prospects in this rapidly developing field. Topics covered include: Discovery and development of fluorine containing drugs and drug candidates. New and efficient synthetic methods for medicinal chemistry and the optimisation of fluorine-containing drug candidates. Structural and chemical biology of fluorinated amino acids and peptides. Fluorine labels as probes in metabolic study, protein engineering and clinical diagnosis. Applications of 19F NMR spectroscopy in biomedical research. An appendix presents an invaluable index of all fluorine-containing drugs that have been approved by the US Food and Drug Administration, including information on structure and pharmaceutical action. Fluorine in Medicinal Chemistry and Chemical Biology will serve as an excellent reference source for graduate students as well as academic and industrial researchers who want to take advantage of fluorine in biomedical research.
Fluorine chemistry is an expanding area of research that is attracting international interest, due to the impact of fluorine in drug discovery and in clinical and molecular imaging (e.g. PET, MRI). Many researchers and academics are entering this area of research, while scientists in industrial and clinical environments are also indirectly exposed to fluorine chemistry through the use of fluorinated compounds for imaging.This book provides an overview of the impact that fluorine has made in the life sciences. In the first section, the emphasis is on how fluorine substitution of amino acids, peptides, nucleobases and carbohydrates can provide invaluable information at a molecular level. The following chapters provide answers to the key questions posed on the importance of fluorine in drug discovery and clinical applications. For examples, the reader will discover how fluorine has found its place as a key element improving drug efficacy, with reference to some of the best-selling drugs on the market. Finally, a thorough review on the design, synthesis and use of 18F-radiotracers for positron emission tomography is provided, and this is complemented with a discussion on how 19F NMR has advanced molecular and clinical imaging./a
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.
Following its well-received predecessor, this book offers an essential guide to chemists for understanding fluorine in spectroscopy. With over 1000 compounds and 100 spectra, the second edition adds new data – featuring fluorine effects on nitrogen NMR, chemical shifts, and coupling constants. • Explains how to successfully incorporate fluorine into target molecules and utilize fluorine substituents to structurally characterize organic compounds • Includes new data on nitrogen NMR, focusing on N-15, to portray the influence of fluorine upon nitrogen NMR chemical shifts and coupling constants • Expands on each chapter from the first edition with additional data and updated discussion from recent findings • "The flawless ordering of material covered in this stand-alone volume is such that information can be found very easily." – Angewandte Chemie review of the first edition, 2010
Fluorine in Life Sciences: Pharmaceuticals, Medicinal Diagnostics and Agrochemicals, volume four in Alain Tressaud's Progress in Fluorine Science series, presents a critical, multidisciplinary overview of the contributions of fluorinated products to solve important global issues in various life science fields, particularly in medicinal chemistry, molecular imaging techniques and agriculture. Edited by recognized experts, this book provides unique coverage of the wide-ranging uses and implications of fluorine and fluorinated compounds. Topics include medicinal monitoring and diagnosis, 19F MRI in medicine and in vivo cell tracking, 18F-labeled radiopharmaceuticals, brain imaging and neurology, risk assessment of reactive metabolites in drug discovery, and more. Edited by Alain Tressaud, past Chair and founder of the CNRS French Fluorine Network, each book in the collection also includes the work of highly-respected volume editors and contributors from both academia and industry who bring valuable and varied content to this active field. - Covers a wide range of topics - from organic and physical chemistry, to pharmaceuticals, agrochemicals and medical diagnostics - Describes major modern syntheses and unique reaction mechanisms yielding fluorine compounds in these diverse life science settings - Features contributions from a wealth of global experts - Acts as the fourth volume in Alain Tressaud's Progress in Fluorine Science
The definitive guide to creating fluorine-based compounds—and the materials of tomorrow Discovered as an element by the French chemist Henri Moissan in 1886, through electrolysis of potassium fluoride in anhydrous hydrogen fluoride—"le fluor," or fluorine, began its chemical history as a substance both elusive and dangerous. With a slight pale yellow hue, fluorine is at room temperature a poisonous diatomic gas. Resembling a spirit from a chemical netherworld, fluorine is highly reactive, difficult to handle, yet very versatile as a reagent—with the power to form compounds with almost any other element. Comprising 20% of pharmaceutical products and 30% of agrochemical compounds, as well as playing a key role in electric cars, electronic devices, and space technology, compounds containing fluorine have grown in importance across the globe. Learning how to safely handle fluorine in the preparation of innovative new materials—with valuable new properties—is of critical importance to chemists today. Bringing together the research and methods of leading scientists in the fluorine field, Efficient Preparations of Fluorine Compounds is the definitive manual to creating, and understanding the reaction mechanisms integral to a wide variety of fluorine compounds. With sixty-eight contributed chapters, the book's extensive coverage includes: Preparation of Elemental Fluorine Synthesis Methods for Exotic Inorganic Fluorides with Varied Applications Introduction of Fluorine into Compounds via Electrophilic and Nucleophilic Reactions Direct Fluorination of Organic Compounds with Elemental Fluorine Efficient Preparations of Bioorganic Fluorine Compounds Asymmetric Fluorocyclization Reactions Preparations of Rare Earth Fluorosulfides and Oxyfluorosulfides The book offers methods and results that can be reproduced by students involved in advanced studies, as well as practicing chemists, pharmaceutical scientists, biologists, and environmental researchers. The only chemical resource of its kind, Efficient Preparations of Fluorine Compounds—from its first experiment to its last—is a unique window into the centuries old science of fluorine and the limitless universe of fluorine-based compounds.
This volume reviews the recent advances in formation of C-F bonds and X-F bonds (X = heteroatom) to produce useful fluorinated molecules for pharmaceuticals, materials and more. Reactions and methods associated with fluorination, including monofluorination, difluorination, trifluorination and other polyfluorination that have emerged within the past few years are systematically discussed. With contributions from front-line researchers in this field from both academia and industry, this book provides a valuable resource for scholars, graduate students as well as professionals.
In view of increasing interest in organofluorine compounds, this book was undertaken to describe biological and physical properties of organofluorine compounds, synthetic methods of these, their roles in pharmaceutical, agrochemical and material sciences. In particular, the book will emphasize on the usefulness of fluorination reaction, availability of fluorination agents, so that even graduate students who are unfamiliar to this field can understand and participate in this fascinating heteroatom chemistry.