Reductive N-alkylation of secondary amines with [2-11C]acetone

Margaretha Van Der Meij, Nicholas I. Carruthers, Jacobus D M Herscheid, Jill A. Jablonowski, Josee E. Leysen, Albert D. Windhorst

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The development of a labeling method for secondary amines with [2- 11C]acetone is described since the R2N-isopropyl moiety is present in many biologically active compounds. The influence of a variety of parameters (e.g. reagents, solvents, temperature, and time) on the reaction outcome is discussed. Under the optimal reaction conditions, [ 11C]1-isopropyl-4-phenylpiperazine ([11C]iPPP) was synthesized from [2-11C]acetone and 1-phenylpiperazine in a decay-corrected radiochemical yield of 72%. The overall synthesis time, from EOB to HPLC analysis of [11C]iPPP, was 20 min. Specific activity was 142-208 GBq/μmol at the end of synthesis.

Original languageEnglish
Pages (from-to)1075-1085
Number of pages11
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Issue number11
Publication statusPublished - 1 Oct 2003


  • Reductive alkylation
  • Reductive amination
  • Secondary amines
  • [2-C]acetone
  • [2-C]tert-butanol

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