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.
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页码：208 / 214
页数：7
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