Synthesis of 18F-labeled neurotensin(8-13) via copper-mediated 1,3-dipolar [3+2] cycloaddition reaction
Synthesis of 18F-labeled neurotensin(8-13) via copper-mediated 1,3-dipolar [3+2] cycloaddition reaction
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DOI：
10.2174/157018007784619998
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发表时间：
2007-06-01
影响因子：
1
通讯作者：
Wuest, Frank
中科院分区：
文献类型：
--
作者：
Ramenda, Theres;Bergmann, Ralf;Wuest, Frank
利用铜(I)介导的末端炔与叠氮化物之间的1，3偶极[3+2]环加成反应，也被称为点击化学，合成了F-18标记的神经降压素(8-13)(NT(8-13))。4-[F-18]氟-N-(丙基-2-炔基)苯甲酰胺[F-18]1作为一种新型的末端炔基构筑块可以成功地与叠氮功能化的NT(8-13)4偶联，得到相应的18F标记的NT(8-13)衍生物[F-18]5，产率为66%。测定了NT(8-13)衍生物[F-19]5的体外结合亲和力为66 nm(IC50)。
The copper(I)-mediated 1,3 dipolar [3+2]cycloaddition between terminal alkynes and azides, also referred to as click-chemistry, was used to synthesize a F-18-labeled neurotensin(8-13) (NT(8-13)). 4-[F-18]Fluoro-N-(prop-2-ynyl)benzamide [F-18]1 as novel terminal alkyne building block could successfully be coupled with azide-functionalized NT(8-13) 4 to give the corresponding 18F-labeled NT(8-13) derivative [F-18]5 in 66% yield as determined by radio-HPLC. The in vitro binding affinity of NT(8-13) derivative [F-19]5 was determined to be 66 nM (IC50).