Author: McCarthy, K.E.

Source: Current Pharmaceutical Design, Volume 6, Number 10, 1 July 2000 , pp. 1057-1083(27)

Publisher: Bentham Science Publishers

Abstract:

Over the past decade, the increased chemical complexity of new drug candidates has resulted in a parallel need to develop innovative syntheses of carbon-14 labelled pharmaceuticals. Faced with short time-lines and a limited number of labelled precursors, radiochemists have addressed this challenge by developing new reagents and adapting existing technology to labelled syntheses. Selected examples from the recent radiochemical literature illustrate some of the creative strategies used to rapidly solve these synthetic challenges. Examples describing the handling and use of common small molecule reagents, such as carbon-14 labelled carbon dioxide, methyl iodide, cyanide, acetic acids, sulfur and phosphorous stabilized ylides for the synthesis of labelled steroids, prostanoids, nucleosides, pyridines, quinolines, benzazepines and other heterocycles are presented. Several general strategies for radiolabelling are also discussed including the degradation strategy for accessing necessary intermediates and precursors, the radiolabelling of aromatic substrates, transition metal mediated cross-couplings, and the use of chiral auxiliaries for the enantioselective syntheses of radiolabelled pharmaceuticals.

Keywords: Carbon 14 labelled; Whole body autoradioluminography; Reagent based; Carbon dioxide; Acetic Acid; Amino acids; Aminoketones; Methyl iodide; Cyanide; Thiocyanate; Formaldehyde; Triethylorthoformated; Diazomethane; Carbon monoxide; Methylphenyl sulfone; Methyl sulfonium salts; Lithiation; Metalhalogen

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1381612003400029

Publication date: 2000-07-01

More about this publication?

• Current Pharmaceutical Design publishes timely in-depth reviews covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area. A Guest Editor who is an acknowledged authority in a therapeutic field has solicits for each issue comprehensive and timely reviews from leading researchers in the pharmaceutical industry and academia.
  
  Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.

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