Details

Autor(en) / Beteiligte

• Zeng, Fanxing
• Voll, Ronald J.
• Crowe, Ronald J.
• Waldrep, Michael S.
• Dolph, Karen B.
• Goodman, Mark M.

Titel

An improved synthesis of [11C]MENET via Suzuki coupling with [11C]methyl iodide

Ist Teil von

• Journal of labelled compounds & radiopharmaceuticals, 2013-05, Vol.56 (5), p.307-309

Ort / Verlag

England: Blackwell Publishing Ltd

Erscheinungsjahr

2013

Quelle

Wiley Online Library All Journals

Beschreibungen/Notizen

• [11C]MENET, a promising norepinephrine transporter imaging agent, was prepared by Suzuki cross coupling of 1 mg N‐t‐Boc pinacolborate precursor with [11C]CH3I in DMF using palladium complex generated in situ from Pd2(dba)3 and (o‐CH3C6H4)3P together with K2CO3 as the co‐catalyst, followed by deprotection with trifluoroacetic acid. This improved radiolabeling method provided [11C]MENET in high radiochemical yield at end of synthesis (EOS, 51 ± 3%, decay‐corrected from end of 11CH3I 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. [11C]MENET, a promising norepinephrine transporter imaging agent, was prepared by Suzuki cross coupling of 1 mg N‐t‐Boc pinacolborate precursor with [11C]CH3I in DMF using palladium complex generated in situ from Pd2(dba)3 and (o‐CH3C6H4)3P together with K2CO3 as the co‐catalyst, followed by deprotection with trifluoroacetic acid. This improved radiolabeling method provided [11C]MENET in high radiochemical yield at end of synthesis (EOS, 51 + 3%, decay‐corrected from end of 11CH3I 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.