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

Author(s): Yoann Joyard, Laurent Bischoff, Vincent Levacher, Cyril Papamicael, Pierre Vera, Pierre Bohn.

Journal Name: Letters in Organic Chemistry

Volume 11 , Issue 3 , 2014

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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 complex 99mTc. However, decomposition of these ligands was observed and we suggest a reasonable explanation based on LC-MS analysis.

Keywords: Technetium-99m, HYNIC, 2-nitroimidazole, tumor hypoxia, imaging, stability evaluation.

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Article Details

Year: 2014
Page: [208 - 214]
Pages: 7
DOI: 10.2174/15701786113106660087
Price: $65

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