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Synthesis and Stability Evaluation of New HYNIC Derivatives as Ligands for Technetium-99m

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An efficient synthetic route to prepare two new HYNIC derivatives with a 2-nitroimidazole moiety designed for tumor hypoxia imaging is described. During the course of the synthesis, the optimization of N-alkylation reaction of 2- nitroimidazole with propargyl bromide is reported to favor the formation of the terminal alkyne versus allene. Thereafter, the two ligands were used with tricine/EDDA to complex99MTc. However, decomposition of these ligands was observed and we suggest a reasonable explanation based on LC-MS analysis.
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Keywords: 2-nitroimidazole; HYNIC; Technetium-99m; imaging; stability evaluation; tumor hypoxia

Document Type: Research Article

Publication date: March 1, 2014

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  • Letters in Organic Chemistry publishes original letters on all areas of organic chemistry including synthesis, bioorganic, medicinal, natural products, organometallic, supramolecular, molecular recognition and physical organic chemistry. The emphasis is placed on publishing quality papers very rapidly. Letters are processed rapidly and take full advantage of the Internet technology both for the submission and the review of the manuscripts.
    The journal is essential reading for all organic chemists both in academia and industry.
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