The design and synthesis of highly branched and spherically symmetric fluorinated macrocyclic chelators
The design and synthesis of highly branched and spherically symmetric fluorinated macrocyclic chelators
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DOI：
10.1055/s-2007-1000857
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发表时间：
2008-01-17
影响因子：
2.6
通讯作者：
Yu, Y. Bruce
中科院分区：
文献类型：
--
作者：
Jiang, Zhong-Xing;Yu, Y. Bruce
设计并高效合成了两种新型的高氟化大环络合剂，它们具有高度支化和球对称的氟碳基团。这是通过将球对称的氟碳部分偶联到大环络合剂DOTA上实现的，在这两个部分之间有或没有柔性低聚氧乙烯连接物。由于具有球对称性，每个氟化螯合剂中的所有27个氟原子都给出了尖锐的单重态F-19核磁共振信号。氟化螯合剂的亲水性和F-19松弛行为可以通过在氟碳部分和大环连接物之间插入柔性连接物来调节。这些螯合剂是H-1-F-19双核核磁共振显像剂的原型。
Two novel, highly fluorinated macrocyclic chelators with highly branched and spherically symmetric fluorocarbon moieties have been designed and efficiently synthesized. This is achieved by conjugating a spherically symmetric fluorocarbon moiety to the macrocyclic chelator DOTA, with or without a flexible oligo-oxyethylene linker between these two parts. As a result of the spherical symmetry, all 27 fluorine atoms in each fluorinated chelator give a sharp singlet F-19 NMR signal. The hydrophilicity and the F-19 relaxation behavior of fluorinated chelators can be modulated by the insertion of a flexible linker between the fluorocarbon moiety and the macrocyclic linker. These chelators serve as prototypes for H-1-F-19 dual nuclei magnetic resonance imaging agents.