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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
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.
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页码:2398 / 2401
页数:4
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