A DIRECT SYNTHESIS OF A BIFUNCTIONAL CHELATING AGENT FOR RADIOLABELING PROTEINS

被引:21
作者
BRECHBIEL, MW
MCMURRY, TJ
GANSOW, OA
机构
[1] Chemistry Section, Radiation Oncology Branch, National Institute of Health, Bethesda
关键词
D O I
10.1016/S0040-4039(00)79202-1
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A convenient synthesis of a bifunctional derivative of the ligand NOTA is described. The synthesis offers advantages over current literature methods for making similar molecules by starting with the easily prepared ortho-amide of 1,4,7-triazacyclononane which can be sequentially alkylated to provide a bifunctional NOTA derivative in 9% yield overall. The replacement of preparative HPLC with simple ion-exchange chromatography provides analytically pure ligand suitable for clinical applications.
引用
收藏
页码:3691 / 3694
页数:4
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