An improved synthesis of [11C]MENET via Suzuki coupling with [11C]methyl iodide. (24th April 2013)

• Record Type: Journal Article
• Authors: Zeng, Fanxing; Voll, Ronald J.; Crowe, Ronald J.; Waldrep, Michael S.; Dolph, Karen B.; Goodman, Mark M.
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 56:Number 5(2013)
• Page Start: 307
• Page End: 309
• Publication Date: 2013-04-24
• Subjects: Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3047
• Languages: English
• ISSNs: 0362-4803

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <p>[¹¹C]MENET, a promising norepinephrine transporter imaging agent, was prepared by Suzuki cross coupling of 1 mg <italic>N‐t</italic>‐Boc pinacolborate precursor with [¹¹C]CH₃I in DMF using palladium complex generated <italic>in situ</italic> from Pd₂(dba)₃ and (<italic>o</italic>‐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, <italic>n</italic> = 6), moderate specific activity (1.5–1.9 Ci/µmol at EOS), and high radiochemical (&gt;98%) and chemical purity (&gt;98%) in a synthesis time of 60 ± 5 min from the end of bombardment. Copyright © 2013 John Wiley &amp; Sons, Ltd.</p> </abstract>