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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 32, Number 6
BKCSDE 32(6)
June 20, 2011

Title	Synthesis of Radioiodinated Carbocyclic Cytosine Analogues
Author	Hyunseok Ahn, Gwangil An, Hakjune Rhee,*,
Keywords	Carbocyclic nucleoside, Radioiodine, PET, Radiopharmaceutical, Labeling
Abstract	The synthesis of carbocyclic analogues of normal nucleosides has grown exclusively since they have shown potential antiviral and antitumor activities. Radiolabeled cis-1-[4-(hydroxy-methyl)-cyclopent-2-enyl]-5-[124I]- iodocytosine (carbocyclic d4IC) and cis-1-[4-(hydroxy-methyl)-cyclopent-2-enyl]-5-(2-[124I]iodovinyl)cytosine (carbocyclic d4IVC) were synthesized. The synthetic route employed Pd(0)-catalyzed coupling reaction together with organotin and exchange reaction for radioiodination as key reactions. Carbocyclic [124I]d4IC gave more than 75% radiochemical yield with greater than 95% radiochemical purity. Carbocyclic [124I]d4IVC gave more than 80% radiochemical yield with greater than 95% radiochemical purity.
Page	1931 - 1935
Full Text	PDF / Supporting Information

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