Synthesis of Radioiodinated Carbocyclic Cytosine Analogues

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-[^(124)I]-iodocytosine (carbocyclic d4IC) and cis-1-[4-(hydroxy-methyl)-cyclopent-2-enyl]-...

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Bibliographic Details
Published in:Bulletin of the Korean Chemical Society 2011, 32(6), , pp.1931-1935
Main Authors: Ahn, Hyun-Seok, An, Gwang-Il, Rhee, Hak-June
Format: Article
Language:English
Subjects:
화학
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Summary: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-[^(124)I]-iodocytosine (carbocyclic d4IC) and cis-1-[4-(hydroxy-methyl)-cyclopent-2-enyl]-5-(2-[^(124)I]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 [^(124)I]d4IC gave more than 75% radiochemical yield with greater than 95% radiochemical purity. Carbocyclic [^(124)I]d4IVC gave more than 80% radiochemical yield with greater than 95% radiochemical purity. KCI Citation Count: 3
ISSN:0253-2964
1229-5949
DOI:10.5012/bkcs.2011.32.6.1931