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Synthesis of Radioiodinated Carbocyclic Cytosine Analogues
- Authors
- Ahn, Hyunseok; An, Gwangil; Rhee, Hakjune
- Issue Date
- Jun-2011
- Publisher
- 대한화학회
- Keywords
- Carbocyclic nucleoside; Radioiodine; PET; Radiopharmaceutical; Labeling
- Citation
- Bulletin of the Korean Chemical Society, v.32, no.6, pp 1931 - 1935
- Pages
- 5
- Indexed
- SCI
SCIE
SCOPUS
KCI
- Journal Title
- Bulletin of the Korean Chemical Society
- Volume
- 32
- Number
- 6
- Start Page
- 1931
- End Page
- 1935
- ISSN
- 0253-2964
1229-5949
- 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-[I-124]-iodocytosine (carbocyclic d4IC) and cis-1[4-(hydroxy-methyl)-cyclopent-2-enyl]-5-(2-[I-124]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 [I-124]d4IC gave more than 75% radiochemical yield with greater than 95% radiochemical purity. Carbocyclic [I-124]d4IVC gave more than 80% radiochemical yield with greater than 95% radiochemical purity.
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Related Researcher
- Rhee, Hak june
- ERICA 공학대학 (ERICA 에너지바이오학과)