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AbstractAbstract
[en] The purpose of this review is to describe the specific application of organotin chemistry to the preparation of radiohalogenated bio-organic compounds as radiotracers. Although the research group was the first to apply the radiohalodestannylation methodology to the synthesis of a labeled compound of biological interest, iodotamoxifen, and subsequently extended its use to the labeled hormones, dopamine receptor antagonists and perfusion agents, the versatility of the method has subsequently found broad acceptance. For many situations in which high specific activity, rapidity of incorporation and labeling site specificity are required, electrophilic destannylation is the method of choice. The sections that follow provide a description of the development of radiohalodestannylation and its application in radiopharmaceutical chemistry. The first section will briefly review the criteria that define the radionuclidic, biochemical and chemical limits associated with radiopharmaceuticals. The next section describes the rationale for the choice of organotin intermediates and highlights the methods available for their synthesis. Following that section are several areas of biomedical research interest that illustrate how organotin chemistry has been applied in the preparation of specific radiohalogenated compounds. Although the examples will focus primarily on situations that require high affinity and specific activity, labeled derivatives which were prepared to evaluate more general physiological properties will also be reviewed. (author). 171 refs
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Buncel, E. (Queen's Univ., Kingston, ON (Canada)); Jones, J.R. (Surrey Univ., Guildford (United Kingdom)) (eds.); Isotopes in the Physical and Biomedical Sciences; v. 1B; 456 p; ISBN 0-444-89186-2;
; 1991; p. 285-340; Elsevier; Amsterdam (Netherlands); GRANT CA19898; GRANT CA31624; GRANT CA41399; CONTRACT DE-FG02-86-ER60460; The author was supported by grants from the U.S. Institute of Health, by contract from the U.s. department of Energy, and by a Research and Scholarship Development Fund Grant from Northeastern University, Boston, MA.

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