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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