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

*Corresponding author for this work

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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

Cite this

Van Der Meij, M., Carruthers, N. I., Herscheid, J. D. M., Jablonowski, J. A., Leysen, J. E., & Windhorst, A. D. (2003). Reductive N-alkylation of secondary amines with [2-11C]acetone. Journal of Labelled Compounds and Radiopharmaceuticals, 46(11), 1075-1085.