Aromatic Fluorination

Aromatic Fluorination PDF

Author: James H. Clark

Publisher: CRC Press

Published: 2018-01-10

Total Pages: 198

ISBN-13: 1351086782

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Academia and industry join forces in Aromatic Fluorination, as an expert from each domain contributes to this new text on fluorination of carbocyclic and heterocyclic rings. The book begins with a discussion of fluorine's unique combination of properties, including size, electronic effects, and hydrophobicity, as well as the historical development of its product applications. It explains methods for introducing fluorine into an aromatic ring, focusing on nucleophilic fluorine transfer reactions. The role of catalysts, solvents, and other variables are examined, and the scope and limitations of the methods are discussed. Of particular interest to those working in non-specialist laboratories, Aromatic Fluorination includes detailed descriptions of the new electrophilic routes to fluoroaromatics, in addition to traditional routes and alternative methods involving radical chemistry. Because one of the most important fluorine-containing substituent is CF3, the book explains routes to benzotrifluorides (ArCF3), including traditional industrial methods and modern alternatives employing C-1 halofluorocarbons and other fluoroaliphatics. An alternative to CF3 is CF3S, and several methods of synthesizing aromatic CF3S-containing molecules are described. Since the successful development and diverse applications of aromatic fluorine compounds have led to the search for new compounds and novel substituents, the incorporation of other substituents is also explored. Aromatic Fluorination concludes with discussion of the factors responsible for the successful development of pharmaceutical, agrochemical and liquid crystal applications and the potential for applications in high-performance polymers and other areas. This section also describes in detail important industrial aromatic fluorination processes and the relative merits of different process technologies and their costs.

Aromatic Fluorination

Aromatic Fluorination PDF

Author: James H. Clark

Publisher: CRC Press

Published: 2018-01-10

Total Pages: 199

ISBN-13: 135107833X

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Describes methods for introducing fluorine and small fluorine-containing substituents into aromatic rings Considers traditional and modern synthetic methods, including industrial processes Focuses on the synthesis of selectively fluorinated aromatic molecules that represent an increasingly important class of intermediates Examines both historical development and future trends in this increasingly important area of chemistry

Fluorine and Health

Fluorine and Health PDF

Author: Alain Tressaud

Publisher: Elsevier

Published: 2008-06-06

Total Pages: 821

ISBN-13: 0080558119

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Fluorine and Health presents a critical multidisciplinary overview on the contribution of fluorinated compounds to resolve the important global issue of medicinal monitoring and health care. The involved subjects are organized in three thematic parts devoted to Molecular Imaging, Biomedical Materials and Pharmaceuticals. Initially the key-position of partially fluorinated low molecular weight compounds labelled either with the natural 19F-isotope for Magnetic Resonance Imaging (MRI) or labelled with the radioactive [18F]-isotope for Positron Emission Tomography (PET) is highlighted. Both non-invasive methods belong to the most challenging in vivo imaging techniques in oncology, neurology and in cardiology for the diagnosis of diseases having the highest mortality in the industrialized countries. The manifold facets of fluorinated biomaterials range from inorganic ceramics to perfluorinated organic molecules. Liquid perfluorocarbons are suitable for oxygen transport and as potential respiratory gas carriers, while fluorinated polymers are connected to the pathology of blood vessels. Another important issue concerns the application of highly fluorinated liquids in ophthalmology. Moreover, fluorine is an essential trace element in bone mineral, dentine and tooth enamel and is applied for the prophylaxis and treatment of dental caries. The various origins of human exposure to fluoride species is detailed to promote a better understanding of the effect of fluoride species on living organisms.Medicinally relevant fluorinated molecules and their interactions with native proteins are the main focus of the third part. New molecules fluorinated in strategic position are crucial for the development of pharmaceuticals with desired action and optimal pharmacological profile. Among the hundreds of marketed active drug components there are more than 150 fluorinated compounds. The chapters will illustrate how the presence of fluorine atoms alters properties of bioactive compounds at various biochemical steps, and possibly facilitate its emergence as pharmaceuticals. Finally the synthetic potential of a fluorinase, the first C-F bond forming enzyme, is summarized. New approach of topics involving chemistry, biology and medicinal techniques Transdisciplinar papers on fluoride products Importance of fluoride products in health Updated data on specific topics

Fluorination

Fluorination PDF

Author: Jinbo Hu

Publisher: Springer

Published: 2020-08-12

Total Pages: 0

ISBN-13: 9789811038952

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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.

Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates

Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates PDF

Author: Al Postigo

Publisher: Elsevier

Published: 2018-09-05

Total Pages: 390

ISBN-13: 0128130393

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Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates reviews how the use of these techniques on compounds with already known and relevant biological activity can provide new pharmaceutical leads with improved medicinal properties. The fluorination strategies discussed take into account both conventional and novel reagents, including nucleophilic, electrophilic, those of a radical nature, and diverse families of organic compounds, such as (hetero) aromatic rings and aliphatic substrates. Drawing on the authors' expert knowledge, this book provides researchers with a broad set of applicable methods to use in their work. Highlights the latest developments in the field in a concise volume Provides details of key fluorinating reagents across diverse families of organic compounds Explores the current applications and future potential of fluorine in drug development

Fluorine in Organic Chemistry

Fluorine in Organic Chemistry PDF

Author: Richard D. Chambers

Publisher: CRC Press

Published: 2004

Total Pages: 426

ISBN-13: 9780849317903

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The introduction of carbon-fluorine bonds into organic compounds can profoundly influence their chemical and physical properties when compared to their non-fluorine-containing analogues, leading to a range of man-made materials with highly desirable properties. These molecules are of interest across the wide spectrum of industrial and academic organic chemistry, from pharmaceuticals, through fine and specialty chemicals to polymers. From Prozac to Teflon, many of the most important products of the chemical and life-science industries rely on organic fluorine chemistry for their useful properties. This book covers both the preparative methodologies and chemical properties of partially and highly fluorinated organic systems.

Nucleophilic Fluorination of Aromatic Compounds

Nucleophilic Fluorination of Aromatic Compounds PDF

Author:

Publisher:

Published: 2014

Total Pages:

ISBN-13:

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Iodylbenzene derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are used as precursors in aromatic nucleophilic substitution reactions. The iodyl group (IO.sub. 2) is regiospecifically substituted by nucleophilic fluoride to provide the corresponding fluoroaryl derivatives. No-carrier-added [F-18]fluoride ion derived from anhydrous [F-18](F/Kryptofix, [F-18]CsF or a quaternary ammonium fluoride (e.g., Me.sub. 4NF, Et.sub. 4NF, n-Bu.sub. 4NF, (PhCH.sub. 2).sub. 4NF) exclusively substitutes the iodyl moiety in these derivatives and provides high specific activity F-18 labeled fluoroaryl analogs. Iodyl derivatives of a benzothiazole analog and 6-iodyl-L-dopa derivatives have been synthesized as precursors and have been used in the preparation of no-carrier-added [F-18]fluorobenzothiazole as well as 6-[F-18]fluoro-L-dopa.

Organic and Inorganic Fluorine Chemistry

Organic and Inorganic Fluorine Chemistry PDF

Author: Axel Haupt

Publisher: Walter de Gruyter GmbH & Co KG

Published: 2021-03-22

Total Pages: 846

ISBN-13: 3110659506

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Organic and Inorganic Fluorine Chemistry provides an introduction to fluorine chemistry and an overview of the most important fluorinated compounds and general preparation techniques. The book is divided into three parts, covering general aspects, inorganic fluorides and fluoroorganic compounds. The inorganic part presents the most important element fluorides and oxyfluorides, their preparation as well as their most characteristic properties. The organic section focuses on the different types of fluorination and the corresponding reagents. The application of these techniques is discussed for many different types of substrates. The book addresses advanced students in chemistry as well as researchers in academia and industry. The readers will benefit from a large number of original references which give access to further information. In addition, study questions at the end of each chapter will help to repeat and internalise the most important aspects.