Synthesis of 1-β-D-(5-Deoxy-5-iodoarabinofuranosyl)-2-nitroimidazole (β-IAZA) : A Novel Marker of Tissue Hypoxia
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概要
- 論文の詳細を見る
The present work describes the synthesis of the β-isomer of 1-α-D-(5-deoxy-5-iodoarabinofuranos>l)-2-ni-truimidazole (IAZA). Radioiodinated IAZA (^<123>I-IAZA) has been extensively studied as a radiopharmaceutical for the diagnosis of regional and/or focal tissue hypoxia in a variety of clinical pathologies. The β-anomer of IAZA, 1-β-D-(5-deoxy-5-iodoarabinofuranosyl)-2-nitroimidazole (β-IAZA, 1), was synthesized via an unconven-ional route starting from 1-β-D-(-(ribofuranosyl)-2-nitroimidazole (AZR), with a change of configuration at the C-2'-position to afford 1-β-D-(-(arabinofuranosyl)-2-nitroimidazole (β-AZA, 7). Nucleophilic iodination of the 5'-O-tolucnesulfonyl-2',3'-di-O-acetyl precursor of β-AZA, 9, followed by deprotection, afforded 1 in satisfactory yield. β-IAZA (I) was also synthesized from 7 using molecular iodine and triphenylphosphine.
- 社団法人日本薬学会の論文
- 2003-04-01
著者
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KUMAR Piyshu
Facultv of Pharmacy & Pharmaceutical Sciences, University of Alberta
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OHKURA Kazue
Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
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BEIKI Davood
Research Institute for Nuclear Medicine, Tehran University of Medical Sciences
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WIEBE Leonard
Facultv of Pharmacy & Pharmaceutical Sciences, University of Alberta
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SEKI Koh-ici
Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
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Kumar Piyshu
Facultv Of Pharmacy & Pharmaceutical Sciences University Of Alberta
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Ohkura Kazue
Faculty Of Pharmaceutical Sciences Health Sciences University Of Hokkaido
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Beiki Davood
Research Institute For Nuclear Medicine Tehran University Of Medical Sciences
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Wiebe Leonard
Facultv Of Pharmacy & Pharmaceutical Sciences University Of Alberta
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Seki Koh-ici
Faculty Of Pharmaceutical Sciences Health Sciences University Of Hokkaido
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Kumar Piyush
Facultv of Pharmacy & Pharmaceutical Sciences, University of Alberta
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OHKURA Kazue
Faculty of Phamaceutical Science, Health Sciences University of Hokkaido
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