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Letters in Organic Chemistry


ISSN (Print): 1570-1786
ISSN (Online): 1875-6255

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 and Pierre Bohn

Volume 11 , Issue 3 , 2014

Page: [208 - 214] Pages: 7

DOI: 10.2174/15701786113106660087

Price: $65


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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