Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates - 1st Edition - ISBN: 9780128129586

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

1st Edition

Authors: Al Postigo
Paperback ISBN: 9780128129586
Imprint: Elsevier
Published Date: 1st October 2018
Page Count: 500
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Fluorination strategies can impact targets of medicinal importance in a range of useful ways, including facilitating modulation of their lipophilicity, electronegativity, basicity and bioavailability. Late Stage Fluorination of Bioactive Molecules reviews how the use of such 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 and those of a radical nature, and diverse families of organic compounds, such as (hetero) aromatic rings and aliphatic substrates.

Drawing on the author’s expert knowledge, this volume provides researchers with a broad set of applicable methods to use in their work, supporting and facilitating the development of novel, enhanced drugs using fluorination strategies.

Key Features

  • Highlights the latest developments in the field in one 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

Table of Contents

  1. Introduction and Highlights
    2. 18F radiolabeling of bioactive compounds
    3. Electrophilic and oxidative fluorination of aromatic compounds
    4. Enantioselective fluorination
    5. Visible-Light-Mediated C-F bond Activation
    6. Photocatalytic fluorination reactions
    7. Fluorination of allylic positions towards the synthesis of fluorinated bioactive compounds
    8. Difluoromethylation of Bioactive Compounds
    9. Fluorination of Bioactive Compounds by Electron Transfer Reactions
    10. Fluorine-Containing Pharmaceuticals and the Phenomenon of Self-Disproportionation of Enantiomers (SDE)


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About the Author

Al Postigo

Professor Postigo has worked at the University of Buenos Aires since 2010, where he teaches in the faculty of pharmacy and biochemistry. Having completed his MSc at the University of Buenos Aires, he then took up a place at McMaster University, Canada, where he completed his Doctoral studies in Organic Chemistry. With a particular research interest in fluorination, he has contributed to over 50 publications across the top journals in the field.

Affiliations and Expertise

Professor of Organic Chemistry, University of Buenos Aires, Argentina

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