The book contains 35 top-notch chapter-reviews on recent methodological developments in the area of synthetic fluoro-organic chemistry based on fluorinated synthons approach. Special emphases are given to the synthesis of biologically relevant compounds (alcohols, amines, alpha- and beta-amino acids, peptides), industrial-scale production of highly versatile, synthetically useful fluorinated synthons, as well as asymmetric synthesis of fluorinated synthons. The book has been designed to be a comprehensive snap-shot of current research activity in the field reviewed by internationally renowned leading experts from academic and industrial laboratories around the world. The topics covered in the book range from synthesis of small fluorinated molecules to peptides and macromolecules for crystal engineering. Substantial amount of data reviewed in the book have never been published. In particular cutting-age technology from industrial laboratories, summarized in the book, will give the reader unprecedented prospective on commercial availability of variety of structurally diverse fluorinated synthons which will be on market in the nearest future. Taking into account the significant impact that fluorinated compounds have made on nearly all aspects of modern life this book is expected to be a current prime reference in the field and might be of interest to diverse readership.

Provides a thorough overview of the role of fluorine in pharmaceutical science and development Includes chapters on fluorinated analogues of natural products, fluorinated amino acids and peptides, and derivatives of sugars Classifies marketed and in-development fluorinated pharmaceuticals according to their therapeutic classes

A thorough survey of synthetic methods, chemistry, and applications of major classes of fluorinated heterocycles Merging organic, heterocyclic, and fluoroorganic chemistry, fluorinated heterocyclic compounds have distinctively desirable properties suitable for use in pharmaceuticals and agrichemicals, especially their ability to penetrate the cell membrane barrier for drug absorption. Offering a needed overview of this relatively new addition to the heterocyclic family, this essential reference provides the latest state-of-the-art information on key application areas within fluorine chemistry. With contributions from experts from both industry and academia, the book covers the chemistry, synthesis, and applications of fluorinated heterocycles with chapters on: Three-, four-, five-, six-, and seven-membered fluorine-containing heterocycles Fluorinated nucleosides Fluorointermediates Applications of fluorinated heterocycles in agricultural products Pharmaceuticals containing fluorinated heterocycles Technical applications of fluorinated heterocycles Written by a team of world-recognized experts in the area of organic and industrial chemistry of fluorine, Fluorinated Heterocyclic Compounds: Synthesis, Chemistry, and Applications will prove valuable to both students and researchers from academia and industry seeking further knowledge of the synthetic methods, chemistry, and applications of major classes of fluorinated heterocycles.

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.

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 two-volume work combines comprehensive information on the chemistry of the fluorinated heterocycles. The material has been divided such that the first volume is dedicated to 5-membered fluorinated heterocycles and macrocycles, while the second volume combines data connected with the chemistry of fluorine containing 6-membered heterocycles. Both volumes will be of interest to synthetic organic chemists in general, and particularly for those colleagues working in the fields of heterocyclic-compound chemistry, materials chemistry, medicinal chemistry, and fluorine chemistry. All information is presented and classified clearly to be effective source for broad auditory of chemists. It will be interesting for scientists working in the field of inorganic and coordination chemistry. Fluorinated heterocycles are becoming increasingly important in many areas including the pharmaceutical industry, materials science and agriculture. The presence of fluorine can result in substantial functional changes in the biological as well as physicochemical properties of organic compounds. Incorporation of fluorine into drug molecules can greatly affect their physicochemical properties, such as bond strength, lipophilicity, bioavailability, conformation, electrostatic potential, dipole moment, pKa etc. as well as pharmacokinetic properties, such as tissue distribution, rate of metabolism and pharmacological properties, such as pharmacodynamics and toxicology.

Fluorine continues to intrigue chemists who overcome the challenge of handling this remarkable halogen and work to develop varied methods for synthesising fluorine compounds. The unique properties of these materials, ranging from inert perfluorocarbons and fluoropolymers to a multitude of other fascinating fluorinated compounds, firmly established their place amidst the technological achievements of the 20th Century. Fluorine substitution in biologically active compounds has become particularly significant in recent years. This book presents new and significant research in this field.

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.

Modern Synthesis Processes and Reactivity of Fluorinated Compounds focuses on the exceptional character of fluorine and fluorinated compounds. This comprehensive work explores examples taken from all classes of fluorine chemistry and illustrates the extreme reactivity of fluorinating media and the peculiar synthesis routes to fluorinated materials. The book provides advanced and updated information on the latest synthesis routes to fluorocompounds and the involved reaction mechanisms. Special attention is given to the unique reactivity of fluorine and fluorinated media, along with the correlation of those properties to valuable applications of fluorinated compounds. - Contains quality content edited, and contributed, by leading scholars in the field - Presents applied guidance on the preparation of original fluorinated compounds, potentially transferable from the lab scale to industrial applications - Provides practical synthesis information for a wide audience interested in fluorine compounds in many branches of chemistry, materials science, and physics

Stereoselective Synthesis of Tetrasubstituted Alkenes via Torquoselectivity-Controlled Olefination of Carbonyl Compounds with Ynolates, by Mitsuru Shindo and Kenji Matsumoto.- Stereoselective Synthesis of Z-Alkenes, by Woon-Yew Siau, Yao Zhang and Yu Zhao.- Stereoselective Synthesis of Mono-fluoroalkenes, by Shoji Hara.- Recent Advances in Stereoselective Synthesis of 1,3-Dienes, by Michael De Paolis, Isabelle Chataigner and Jacques Maddaluno.- Selective Olefination of Carbonyl Compounds via Metal-Catalyzed Carbene Transfer from Diazo Reagents, by Yang Hu and X. Peter Zhang.- Selective Alkene Metathesis in the Total Synthesis of Complex Natural Product, by Xiaoguang Lei and Houhua Li.- Olefination Reactions of Phosphorus-Stabilized Carbon Nucleophiles, by Yonghong Gu and Shi-Kai Tian.- Alkene Synthesis Through Transition Metal-Catalyzed Cross-Coupling of N-Tosylhydrazones, by Yan Zhang and Jianbo Wang.