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Reductive N ‐alkylation of secondary amines with [2‐ 11 C]acetone
Author(s) -
van der Meij Margaretha,
Carruthers Nicholas I.,
Herscheid Jacobus D.M.,
Jablonowski Jill A.,
Leysen Josee E.,
Windhorst Albert D.
Publication year - 2003
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.740
Subject(s) - chemistry , acetone , alkylation , reagent , yield (engineering) , isopropyl , moiety , chemical synthesis , specific activity , organic chemistry , radiochemistry , catalysis , in vitro , biochemistry , materials science , metallurgy , enzyme
The development of a labeling method for secondary amines with [2‐ 11 C]acetone is described since the R 2 N ‐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, [ 11 C]1‐isopropyl‐4‐phenylpiperazine ([ 11 C]iPPP) was synthesized from [2‐ 11 C]acetone and 1‐phenylpiperazine in a decay‐corrected radiochemical yield of 72%. The overall synthesis time, from EOB to HPLC analysis of [ 11 C]iPPP, was 20 min. Specific activity was 142–208 GBq/μmol at the end of synthesis. Copyright © 2003 John Wiley & Sons, Ltd.