Synthesis of 2'-deoxy-2'-[18F]fluoro-beta-D-arabinofuranosyl nucleosides, [18F]FAU, [18F]FMAU, [18F]FBAU and [18F]FIAU, as potential PET agents for imaging cellular proliferation. Synthesis of [18F]labelled FAU, FMAU, FBAU, FIAU.
An efficient and reliable synthesis of 2'-deoxy-2'-[(18)F]fluoro-beta-D-arabinofuranosyl nucleosides is presented. Overall decay-corrected radiochemical yields of 35-45% of 4 analogs, FAU, FMAU, FBAU and FIAU are routinely obtained in >98% radiochemical purity and with specific activities of greater than 3 Ci/micromol (110 MBq/micromol) in a synthesis time of approximately 3 hours. When approximately 220 mCi (8.15 GBq) of starting [(18)F]fluoride is used, 25 -30 mCi (0.93 -1.11 GBq) of product (enough to image two patients sequentially) is typically obtained.
Mangner
Thomas J
TJ
Children's Hospital of Michigan, PET Center, Wayne State University, Detroit, MI 48201, USA. tmangner@pet.wayne.edu
Klecker
Raymond W
RW
Anderson
Lawrence
L
Shields
Anthony F
AF
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry; D001086:Arabinofuranosyluracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D001087:Arabinonucleosides / Q000138:chemical synthesis* / Q000737:chemistry; D005462:Fluorine Radioisotopes
C457880:2'-fluorodeoxyuracil-arabinofuranoside; D000998:Antiviral Agents; D001087:Arabinonucleosides; D005462:Fluorine Radioisotopes; D001086:Arabinofuranosyluracil; C043457:fialuridine; C034935:clevudine