Synthesis of a DOTA-Biotin Conjugate for Radionuclide Chelation via Cu-Free Click Chemistry

被引：54
|
作者：
Schultz, Michael K. [1 ,2 ]
Parameswarappa, Sharavathi G. [3 ]
Pigge, F. Christopher [3 ]
机构：
[1] Univ Iowa, Carver Coll Med, Dept Radiol, Iowa City, IA 52242 USA
[2] Univ Iowa, Carver Coll Med, Dept Radiat Oncol, Iowa City, IA 52242 USA
[3] Univ Iowa, Dept Chem, Iowa City, IA 52242 USA
来源：
ORGANIC LETTERS | 2010年 / 12卷 / 10期
关键词：
FREE TRIAZOLE FORMATION; COPPER-FREE; 1,3-DIPOLAR CYCLOADDITION; SOMATOSTATIN ANALOG; TERMINAL ALKYNES; AZIDES; RADIOPHARMACEUTICALS; PET;
D O I：
10.1021/ol100774p
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A strain-induced copper-free click reaction mediated by a new and easily prepared cyclooctyne derivative was used to efficiently assemble a DOTA biotin adduct capable of radionuclide ((68)Ga) uptake. This synthetic strategy offers a potentially general and convenient means of preparing targeted radiolabeling and radiotherapeutic agents.
引用
收藏
页码：2398 / 2401
页数：4
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