Synthesis of Radioiodinated Carbocyclic Cytosine Analogues

Title
Synthesis of Radioiodinated Carbocyclic Cytosine Analogues
Author
이학준
Keywords
Carbocyclic nucleoside; Radioiodine; PET; Radiopharmaceutical; Labeling
Issue Date
2011-06
Publisher
Korean Chemical Society
Citation
Bulletin of the Korean Chemical Society, v.32, no.6.2011년, pp.1931 - 1935
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-$[^{124}I]$-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.
URI
http://koreascience.or.kr/article/ArticleFullRecord.jsp?cn=JCGMCS_2011_v32n6_1931
ISSN
0253-2964
DOI
10.5012/bkcs.2011.32.6.1931
Appears in Collections:
GRADUATE SCHOOL[S](대학원) > BIONANOTECHNOLOGY(바이오나노학과) > Articles
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