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

ISBN-10: 1402045603

ISBN-13: 9781402045608

ISBN-10: 1402045611

ISBN-13: 9781402045615

This compendium describes the foremost creation routes of the six such a lot proper iodine radio isotopes and a number of the tools of labeling molecules of organic, diagnostic or pharmaceutical curiosity with them. The chapters describe the elemental response mechanisms, and the impact of iodine creation on physical/chemical and pharmacological houses. They contain examples of significant response pathways for the coaching of radio-iodine compounds.

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

Sample text

The quality of a tracer for functional imaging will be mostly related to the balance of performance of the tracer in these two phases. This makes what is called development of ‘‘smart radiopharmaceuticals’’. The distribution of a radiopharmaceutical is usually expressed by its volume of distribution (VD) and indicates the virtual blood volume calculated from the (remaining) concentration in blood and from the total administered doses of activity. It is a theoretical number that assumes the radiopharmaceutical is at uniform concentration in the tissue and in the circulation (blood flow).

Radioiodine-for-Bromine or -Chlorine Exchange The SN Ar reactions can be accelerated by using particular drastic conditions. For example, the radioiodination of a potential MAO-A ligand, Ro 119900, an iodinated analogue of moclobemide, was easily achieved under solidstate conditions in ammonium sulphate using the brominated precursor and [125 I]NaI at 2108C for 40 min [47]. The iodine-for-bromine exchange technique was successfully used for the radioiodination of benzodiazepines [48,49], L-6-iododopa (6-ID) [50] and benzamide [51].

J Med Chem 39:543–548 Goodman MM, Kung MP, Kabalka GW, Kung HF, Switzer R (2002) Synthesis and characterization of radioiodinated N-(3-iodopropen-1-yl)-2b-carbomethoxy-3b-(4chlorophenyl)tropanes: potential dopamine reuptake site imaging agents. J Med Chem 37:1535–1542 Frangin Y, Caillet M, Chalon S (1990) A new method to prepare no-carrier-added iodinated spirodecanone derivatives: applications to dopaminergic and serotoninergic ligands. J Label Comp Radiopharm 28:1363–1373 Hamant S, Mathieu J-P, Morin C, Trimcev I, Vidal M (1994) The b-iodoethyl group: a stable unit for radioiodination.

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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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