Fluorine in life sciences : pharmaceuticals, medicinal diagnostics, and agrochemicals /: pharmaceuticals, medicinal diagnostics, and agrochemicals. ([2019])

• Record Type: Book
• Further Information: Note: Edited by Günter Haufe, Frédéric R. Leroux.
• Editors: Haufe, Günter; Leroux, Frederic
• Contents: 4.3.1 Fluorination of the a-position of carbonyl compounds4.3.2 Electrophilic fluorination of enolates; 4.4 From carboxylic acids; 4.5 From diazo compounds/olefins; 5. Aromatic C-H fluorination; 5.1 Electrophilic aromatic fluorination; 5.2 Transition metal-catalyzed aromatic C-H fluorination; 6. Benzylic C-H fluorination; 6.1 Transition metal-catalyzed C-H fluorination; 6.2 Metal free-radical initiated fluorination; 6.3 Photocatalyzed C-H fluorination; 7. Fluorination of unactivated aliphatic C-H bonds; 7.1 Transition metal-catalyzed C-H fluorination; 7.2 Radical-initiated fluorination. 3.3 Transition metal-catalyzed fluorination of aryl halides and pseudo-halides3.4 Aromatic deoxyfluorination: PhenoFluor/PhenoFluor Mix; 3.5 Decarboxylative fluorination of heterocycles; 3.6 Fluorination of aryl boron derivatives; 3.7 Fluorination of aryl stannanes; 3.8 Fluorination of aryl silanes; 3.9 Fluorination of diaryliodonium salts; 4. Fluorination of prefunctionalized aliphatic substrates; 4.1 Nucleophilic displacement of halides/activated alcohols; 4.2 Deoxyfluorination-a new era!; 4.3 Direct replacement from aldehydes/ketones. 7.3 Photocatalyzed fluorination of unactivated aliphatic C-H bonds8. Conclusions and outlook; References; 2 -- Fluorination patterns in small alkyl groups: their impact on properties relevant to drug discovery; 1. Introduction; 2. Effective and intrinsic lipophilicity; 3. Basicity modulation by fluorine in aliphatic amines; 4. Modulation of lipophilicity by partially fluorinated alkyl groups; 5. Partially fluorinated alkyl groups attached to aryl carbon; 6. Partially fluorinated alkyl groups attached to ether oxygen; 7. Partially fluorinated alkyl groups attached to saturated amine nitrogen. 8. Aqueous solubility related to lipophilicity and crystal lattice energy9. In vitro oxidative metabolism related to lipophilicity; 10. Conclusions and outlook; References; 3 -- Polyfluorinated scaffolds in drug discovery; 1. Introduction; 1.1 Properties of fluorine; 2. Fluorine chemistry and drug discovery; 2.1 Fluorinated natural products; 2.2 "Early" perfluoroalkyl group-containing compounds; 2.3 Metabolism and toxicity of polyfluorinated compounds; 3. Polyfluorinated drugs; 3.1 Central nervous system agents; 3.2 Anticancer agents; 3.3 Metabolic disorder agents. Front Cover; Fluorine in Life Sciences:Pharmaceuticals, Medicinal Diagnostics, and Agrochemicals; Fluorine in Life Sciences:Pharmaceuticals, Medicinal Diagnostics, and Agrochemicals; Contents; List of contributors; About the editors; Preface; 1 -- Emerging fluorination methods in organic chemistry relevant for life science application; 1. Introduction; 2. Common reagents; 2.1 Nucleophilic fluorination sources; 2.2 Electrophilic fluorination sources; 3. Fluorination of prefunctionalized aromatic/heteroaromatic substrates; 3.1 Balz-Schiemann reaction; 3.2 The Halex reaction.
• Publisher Details: London, United Kingdom San Diego, CA : Academic Press
• Publication Date: 2019
• Extent: 1 online resource (xviii, 667 pages)
• Subjects: 546/.731; Fluorine; Fluorine -- Physiological effect; SCIENCE -- Chemistry -- Inorganic; Fluorine; Fluorine -- Physiological effect; Electronic books
• Languages: English
• ISBNs: 9780128127346; 0128127341
• Related ISBNs: 9780128127339; 0128127333
• Notes: Note: Includes bibliographical references and index.; Note: Description based on online resource; title from digital title page (viewed on April 24, 2019).
• Access Rights: Legal Deposit; Only available on premises controlled by the deposit library and to one user at any one time; The Legal Deposit Libraries (Non-Print Works) Regulations (UK).
• Access Usage: Restricted: Printing from this resource is governed by The Legal Deposit Libraries (Non-Print Works) Regulations (UK) and UK copyright law currently in force.