Abstract
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.
Letters in Organic Chemistry
Title:Synthesis and Stability Evaluation of New HYNIC Derivatives as Ligands for Technetium-99m
Volume: 11 Issue: 3
Author(s): Yoann Joyard, Laurent Bischoff, Vincent Levacher, Cyril Papamicael, Pierre Vera and Pierre Bohn
Affiliation:
Keywords: Technetium-99m, HYNIC, 2-nitroimidazole, tumor hypoxia, imaging, stability evaluation.
Abstract: 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.
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Cite this article as:
Joyard Yoann, Bischoff Laurent, Levacher Vincent, Papamicael Cyril, Vera Pierre and Bohn Pierre, Synthesis and Stability Evaluation of New HYNIC Derivatives as Ligands for Technetium-99m, Letters in Organic Chemistry 2014; 11 (3) . https://dx.doi.org/10.2174/15701786113106660087
DOI https://dx.doi.org/10.2174/15701786113106660087 |
Print ISSN 1570-1786 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6255 |
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