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

被引：3

作者：

Joyard, Yoann ^{[1
,2
,3
,4
]}

Bischoff, Laurent ^{[4
]}

Levacher, Vincent ^{[4
]}

Papamicel, Cyril ^{[4
]}

Vera, Pierre ^{[1
,2
,3
]}

Bohn, Pierre ^{[1
,2
,3
]}

机构：

[1] Ctr Henri Becquerel, Dept Nucl Med, F-76038 Rouen, France

[2] Rouen Univ Hosp, F-76038 Rouen, France

[3] QuantIF LITIS, EA4108, F-76038 Rouen, France

[4] IRCOF Rouen, F-76130 Mont St Aignan, France

来源：

LETTERS IN ORGANIC CHEMISTRY | 2014年 / 11卷 / 03期

关键词：

Technetium-99m; HYNIC; 2-nitroimidazole; tumor hypoxia; imaging; stability evaluation; HYPOXIA IMAGING AGENT; IN-VIVO EVALUATION; TUMOR HYPOXIA; IODOAZOMYCIN ARABINOSIDE; FOCAL SITES; COMPLEX; BIODISTRIBUTION; INFECTION; ANALOGS; MARKER;

D O I：

10.2174/15701786113106660087

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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 Tc-99m. However, decomposition of these ligands was observed and we suggest a reasonable explanation based on LC-MS analysis.

引用

页码：208 / 214

页数：7

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