Journal
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
Volume 46, Issue 11, Pages 1075-1085Publisher
WILEY
DOI: 10.1002/jlcr.740
Keywords
[2-C-11]acetone; reductive alkylation; reductive amination; secondary amines; [2-C-11]tert-butanol
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The development of a labeling method for secondary amines with [2-C-11]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, [C-11]1-isopropyl-4-phenylpiperazine ([C-11]iPPP) was synthesized from [2-C-11]acetone and 1-phenylpiperazine in a decay-corrected radiochemical yield of 72%. The overall synthesis time, from EOB to HPLC analysis of [C-11]iPPP, was 20 min. Specific activity was 142-208 GBq/mumol at the end of synthesis. Copyright (C) 2003 John Wiley Sons, Ltd.
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