[18F]Fluoropropylsulfonyl chloride: A new reagent for radiolabeling primary and secondary amines for PET imaging

Zheng Li, Lixin Lang, Ying Ma, Dale O. Kiesewetter

Research output: Contribution to journalArticle

7 Scopus citations

Abstract

In vivo molecular imaging with positron emission tomography (PET) requires the preparation of an appropriate positron-emitting radiotracer. New methods for the introduction of F-18 into biologically interesting molecules could increase the availability of specific PET radiotracers and increase the application of PET to the study of human diseases. In this work, [18F] fluoropropylsulfonyl chloride was synthesized from 3-toluenesulfonyloxypropyl thiocyanate in two steps and was successfully incorporated into molecules containing a reactive amino group. Both a primary amine, L-phenylalanine ethyl ester hydrochloride, and a secondary amine, 1-(2-methoxyphenyl)-piperazine, were successfully radiolabeled by this method. The entire radiochemical synthesis required 90 min. The products were obtained in 25.7 ± 2.3% (n = 3) and 22.8 ± 9.1% (n = 6) (EOB). This method provides a useful and easy way to make new F-18 labeled radiopharmaceuticals for PET imaging.

Original languageEnglish (US)
Pages (from-to)23-27
Number of pages5
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume51
Issue number1
DOIs
StatePublished - Jan 1 2008

Keywords

  • [f]fluoropropylsulfonyl chloride
  • Fluorine-18
  • Radiolabeling agent

ASJC Scopus subject areas

  • Analytical Chemistry
  • Drug Discovery
  • Organic Chemistry
  • Clinical Biochemistry
  • Molecular Medicine
  • Pharmacology

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