title: An improved synthesis of [11C]MENET via Suzuki coupling with [11C]methyl iodide.
abstract: [(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]CH3 I in DMF using palladium complex generated in situ from Pd2 (dba)3 and (o-CH3 C6 H4 )3 P together with K2 CO3 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) CH3 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.
authors.affiliation: Department of Radiology and Imaging Sciences, Emory University, 1841 Clifton Road NE, Atlanta, GA, 30329, USA.
authors.forename: Fanxing
authors.initials: F
authors.lastname: Zeng
authors.forename: Ronald J
authors.initials: RJ
authors.lastname: Voll
authors.forename: Ronald J
authors.initials: RJ
authors.lastname: Crowe
authors.forename: Michael S
authors.initials: MS
authors.lastname: Waldrep
authors.forename: Karen B
authors.initials: KB
authors.lastname: Dolph
authors.forename: Mark M
authors.initials: MM
authors.lastname: Goodman
mesh_terms: D002250:Carbon Radioisotopes / Q000737:chemistry; D007553:Isotope Labeling / Q000379:methods*; D009025:Morpholines / Q000138:chemical synthesis* / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*
chemical_list: C000589727:2-(alpha-(2-methylphenoxy)phenylmethyl)morpholine; D002250:Carbon Radioisotopes; D009025:Morpholines; D019275:Radiopharmaceuticals
keywords: Suzuki coupling; [11C]MENET; carbon-11; pinacolborate