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Synthesis of 18F-labeled neurotensin(8-13) via copper-mediated 1,3-dipolar [3+2]cycloaddition reaction

Ramenda, T.; Bergmann, R.; Wüst, F.
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 18F-labeled neurotensin(8-13) (NT(8-13)). 4-[18F]Fluoro-N-(prop-2-ynyl)benzamide [18F]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 [18F]5 product in 66% yield as determined by radio-HPLC. The in vitro binding affinity of 18F-labeled NT(8-13) derivative [18F]5 was determined to be 66 nM.
  • Letters in Drug Design & Discovery 4(2007)4, 279-285

Permalink: https://www.hzdr.de/publications/Publ-9005
Publ.-Id: 9005