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

…, L Bischoff, V Levacher, C Papamicaël…

Index: Joyard, Yoann; Bischoff, Laurent; Levacher, Vincent; Papamicael, Cyril; Vera, Pierre; Bohn, Pierre Letters in Organic Chemistry, 2014 , vol. 11, # 3 p. 208 - 214

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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 complex99MTc. However, decomposition of these ...