Click for PET: rapid preparation of [18F]fluoropeptides using CuI catalyzed 1,3-dipolar cycloaddition

Jan Marik, Julie Sutcliffe

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Abstract

CuI catalyzed 1,3-dipolar cycloaddition 'click chemistry' was used to prepare 18F-radiolabeled peptides. Three ω-[18F]fluoroalkynes were prepared in yields ranging from 36% to 81%. Conjugation of ω-[18F]fluoroalkynes to various peptides decorated with 3-azidopropionic acid via CuI mediated 1,3-dipolar cycloaddition yielded the desired 18F-labeled products in 10 min with yields of 54-99% and excellent radiochemical purity (81-99%). The total synthesis time was 30 min from the end of bombardment.

Original languageEnglish (US)
Pages (from-to)6681-6684
Number of pages4
JournalTetrahedron Letters
Volume47
Issue number37
DOIs
StatePublished - Sep 11 2006

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ASJC Scopus subject areas

  • Biochemistry
  • Organic Chemistry
  • Drug Discovery

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