Download e-book for iPad: Radioionidation Reactions for Pharmaceuticals: Compendium by H.H. Coenen, John Mertens, Bernard Mazière

By H.H. Coenen, John Mertens, Bernard Mazière

ISBN-10: 1402045603

ISBN-13: 9781402045608

ISBN-10: 1402045611

ISBN-13: 9781402045615

This compendium describes the main creation routes of the six so much correct iodine radio isotopes and many of the equipment of labeling molecules of organic, diagnostic or pharmaceutical curiosity with them. The chapters describe the elemental response mechanisms, and the effect of iodine advent on physical/chemical and pharmacological houses. They comprise examples of significant response pathways for the instruction of radio-iodine compounds.

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Extra info for Radioionidation Reactions for Pharmaceuticals: Compendium for Effective Synthesis Strategies

Example text

72] propagate a primary complexation of Cu in a higher oxidation state with the carbon–halogen bond of the precursor with subsequent nucleophilic substitution by radioiodide. Some observations make even a pure nucleophilic mechanism appear doubtful. Moerlein [58] found a decrease of substitution yield with less electron-withdrawing (activating) substituents but an increase with electron-donating (deactivating) substituents and also lowest yields with fluorine as nucleofugic group, both effects contradicting nucleophilic substitution.

Radioiodination via nucleophilic substitution is most often performed with aliphatic and aromatic compounds according to the nature of the leaving group. 2 Halogen Exchange in Aliphatic Compounds In aliphatic compounds, the reactions occur at a saturated carbon atom and correspond to the most common SN 1 and SN 2 mechanisms. The parameters affecting these reaction types such as properties of the compound, nucleophile, leaving group, solvent temperature, kinetics and stereochemistry are discussed in detail in basic teaching books.

J Label Comp Radiopharm 19:1103–1109 [102] Foster NI, Heindel ND, Burns HD, Muhr W (1980) Aryl iodides from anilines via triazene intermediates. Synthesis 1:572–573 [103] Ku H, Barrio JR (1981) Convenient synthesis of aryl halides fromarylamines via treatment of 1-aryl-3,3-dialkyltriazenes with trimethylsilyl halides. J Org Chem 46:5239–5241 [104] Goodman MM, Knapp FF, Callahan AP, Ferren LA (1982) Radioiodinated 15-( piodophenyl)-6-tellurapentadecanoic acid: a new agent showing prolonged myocardial retention.

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Radioionidation Reactions for Pharmaceuticals: Compendium for Effective Synthesis Strategies by H.H. Coenen, John Mertens, Bernard Mazière

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