| Description |
1 online resource (xviii, 667 pages) |
| Series |
Progress in fluorine science series |
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Progress in fluorine science series.
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| 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 |
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880-01 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 |
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880-01/(S 4.3.1 Fluorination of the α-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 |
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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 |
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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 |
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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 |
| Bibliography |
Includes bibliographical references and index |
| Notes |
3.3.1 Fenfluramine (1973, 70) and Tiflorex (Flutiorex, 71) |
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Online resource; title from digital title page (viewed on April 24, 2019) |
| Subject |
Fluorine.
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Fluorine -- Physiological effect.
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Fluorine -- pharmacology
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Fluorine
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SCIENCE -- Chemistry -- Inorganic.
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Fluorine
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Fluorine -- Physiological effect
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| Form |
Electronic book
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| Author |
Haufe, Günter, editor.
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Leroux, Frederic, editor
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| ISBN |
9780128127346 |
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0128127341 |
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