Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Synthesis of 18F-labeled Neurotensin(8-13) via Copper-Mediated 1,3-Dipolar [3+2]Cycloaddition Reaction

Author(s): Theres Ramenda, Ralf Bergmann, Frank Wuest.

Abstract:

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 in 66% yield as determined by radio-HPLC. The in vitro binding affinity of NT(8-13) derivative [19F]5 was determined to be 66 nM (IC50 ).

Keywords: Click chemistry, 18F-labeling, Neurotensin, Positron emission tomography (PET)

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Article Details

VOLUME: 4
ISSUE: 4
Year: 2007
Page: [279 - 285]
Pages: 7
DOI: 10.2174/157018007784619998
Price: $58