Synthesis and Stability Evaluation of New HYNIC Derivatives as Ligands for Technetium-99m
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.
Keywords: 2-nitroimidazole; HYNIC; Technetium-99m; imaging; stability evaluation; tumor hypoxia
Document Type: Research Article
Publication date: 01 March 2014
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