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Manual Radioionidation Reactions for Pharmaceuticals: Compendium for Effective Synthesis Strategies

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Emmanuel s. Feldstein, Paul J. Gareth A. Grubb, Philip W. Hardee, Gregory E. Hefter, G. Heinz H. Hersh, William R. Herzlinger, Regina E. James A. Jass, Jana. Johnson, I. Joseph D. Kim Huynh-Ba, ed. Kucers, A. Kuntze, Marcus F. Kwon, Younggil. Laurence S. Lauro, Gabriel J. Letovsky, Stanley. Mann, Ronald D. Mansoor M. Mount, David W. Nasser H. Ohannesian, Lena. Parker, James N. Parker, Philip M. Peter, K. Volume 2. Pirsch, John. Priebe, Stefan; Slade, Mike. Puri, Harbans Singh. Regine Eibl, et al.


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Physical properties and areas of application. Radiochemical and radionuclidic purity. Specific radioactivity.


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Production of iodine radionuclides. Production of I. Physico-chemical properties. Carbon-iodine bond. Bond distances. Energy, stability. Steric hindrance and electronic density. Pharmaceutical properties.

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Chemical and radiochemical purity. Stability in vitro and shelf-life. Pharmacological characteristics. Pharmaceutical considerations. Nucleophilic substitution. Halogen exchange in aliphatic compounds. Isotopic exchange.

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Radioiodine-for-bromine exchange. Halogen exchange in aromatic compounds. Radioiodine-for-bromine or -chlorine exchange. Copper assisted halogen exchange. Cu I assisted radioiodination. Cu II assisted radioiodination. Electrophilic substitution.

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General considerations. Oxidising reagents. Iodine monohalide ICl, IF. Iodogen t N-Halosuccinimides. Other oxidants. Direct electrophilic radioiodination radioiodo- deprotonation. Demetallation techniques radioiodo-demetallation. Radioiodo-demetallation with group IV metals.

Coenen, Heinz H.

Radioiodo-demetallation with mercury and thallium. Macromolecule labelling. Protein radioiodination. Direct radioiodination of proteins. Indirect radioiodination. Amine-reactive conjugates. Sulfhydryl-reactive conjugates. Carbohydrate-reactive conjugates. Nonspecific conjugates. Oligonucleotide radioiodination.