title: Radiosynthesis of F-18 labeled cytidine analog 2'-fluoro-5-iodo-l-beta-d-arabinofuranosylcytosine ([(18)F]FIAC).
abstract: We reported the synthesis of 2'-deoxy-2'-[(18)F]fluoro-5-iodo-1-beta-d-arabinofuranosyl-5-iodo-cytosine ([(18)F]FIAC) with 15-20% radiochemical yield (decay corrected) in 3.5h. 2-deoxy-2-[(18)F]fluoro-1,3,5-tri-O-benzoyl-alpha-d-arabinofuranose was prepared following literature procedures with some modifications (yield>70%). The (18)F-fluorosugar was converted to 1-bromo-(18)F-fluorosugar, and then coupled with 5-iodocytocine silyl ether. A mixture of acetonitrile (ACN) and 1,2-dichloroethane (DCE) were employed to achieve optimum radiochemical yield and acceptable beta-anomer selectivity (alpha/beta=1/3). After hydrolyzed with sodium methoxide, the crude product was purified using HPLC to afford the beta-[(18)F]FIAC with high radiochemical purity (>or=98%).
authors.affiliation: Institute of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, 155, Li-Nong Street, Sector 2, Bei-tou, Taipei 112, Taiwan.
authors.forename: Chun-Yi
authors.initials: CY
authors.lastname: Wu
authors.forename: Pei-Chia
authors.initials: PC
authors.lastname: Chan
authors.forename: Wei-Ting
authors.initials: WT
authors.lastname: Chang
authors.forename: Ren-Shyan
authors.initials: RS
authors.lastname: Liu
authors.forename: Mian M
authors.initials: MM
authors.lastname: Alauddin
authors.forename: Hsin-Ell
authors.initials: HE
authors.lastname: Wang