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An improved synthesis of [ 11 C]MENET via Suzuki coupling with [ 11 C]methyl iodide
Author(s) -
Zeng Fanxing,
Voll Ronald J.,
Crowe Ronald J.,
Waldrep Michael S.,
Dolph Karen B.,
Goodman Mark M.
Publication year - 2013
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.3047
Subject(s) - chemistry , trifluoroacetic acid , yield (engineering) , iodide , palladium , chemical synthesis , methyl iodide , suzuki reaction , catalysis , radiochemistry , specific activity , nuclear chemistry , medicinal chemistry , organic chemistry , in vitro , biochemistry , materials science , metallurgy , enzyme
[ 11 C]MENET, a promising norepinephrine transporter imaging agent, was prepared by Suzuki cross coupling of 1 mg N‐t ‐Boc pinacolborate precursor with [ 11 C]CH 3 I in DMF using palladium complex generated in situ from Pd 2 (dba) 3 and ( o ‐CH 3 C 6 H 4 ) 3 P together with K 2 CO 3 as the co‐catalyst, followed by deprotection with trifluoroacetic acid. This improved radiolabeling method provided [ 11 C]MENET in high radiochemical yield at end of synthesis (EOS, 51 ± 3%, decay‐corrected from end of 11 CH 3 I synthesis, n = 6), moderate specific activity (1.5–1.9 Ci/µmol at EOS), and high radiochemical (>98%) and chemical purity (>98%) in a synthesis time of 60 ± 5 min from the end of bombardment. Copyright © 2013 John Wiley & Sons, Ltd.