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.
Subject(s)
Isotope Labeling/methods , Morpholines/chemical synthesis , Radiopharmaceuticals/chemical synthesis , Carbon Radioisotopes/chemistry , Morpholines/chemistryABSTRACT
The fluorine-18 labeled dopamine transport (DAT) ligand 2 beta-carbomethoxy-3beta-(4-chlorophenyl)-8-(2-fluoroethyl)nortropane (FECNT) has shown promising properties as an in vivo DAT imaging agent in human and monkey PET studies. A semi-automated synthesis has been developed to reliably produce [(18)F]FECNT in a 16% decay corrected yield. This method utilizes a new [(18)F]fluoralkylating agent and provides high purity [(18)F]FECNT in a formulation suitable for human use.
