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タイトル: The synthesis of [18F]pitavastatin as a tracer for hOATP using the Suzuki coupling.
著者: Yagi, Yusuke
Kimura, Hiroyuki
Arimitsu, Kenji
Ono, Masahiro
Maeda, Kazuya
Kusuhara, Hiroyuki
Kajimoto, Tetsuya
Sugiyama, Yuichi
Saji, Hideo
著者名の別形: 木村, 寛之
佐治, 英郎
発行日: 13-Nov-2014
出版者: Royal Society of Chemistry
誌名: Organic & biomolecular chemistry
巻: 13
号: 4
開始ページ: 1113
終了ページ: 1121
抄録: Fluorine-18 labeled radiotracers, such as [(18)F]fluorodeoxyglucose, can be used as practical diagnostic agents in positron emission tomography (PET). Furthermore, the properties of pharmaceuticals can be enhanced significantly by the introduction of fluorine groups into their original structures, and significant progress has been made during the last three decades towards the development of practical procedures for the introduction of fluorine. The replacement of the fluorine atoms present in pharmaceuticals with radioactive (18)F atoms is a rational approach for designing novel PET tracers. As a fluorine-containing pharmaceutical agent, pitavastatin has attracted considerable interest from researchers working in the life sciences because it can act as an antihyperlipidemic agent as well as a substrate for hepatic organic anion transporting polypeptides (hOATP). With this in mind, it was envisaged that [(18)F]pitavastatin would be used as an excellent imaging agent for hOATP, which prompted us to investigate the synthesis of this agent. Herein, we report a practical method for the synthesis of [(18)F]pitavastatin by the Suzuki coupling reaction of p-iodofluorobenzene and a quinoline boronate derivative, with the desired product being formed in a radiochemical yield of 12 ± 3% (decay corrected from [(18)F]fluoride ions, n = 3).
著作権等: © The Royal Society of Chemistry 2015
許諾条件により本文ファイルは2015-11-13に公開.
This is not the published version. Please cite only the published version. この論文は出版社版でありません。引用の際には出版社版をご確認ご利用ください。
URI: http://hdl.handle.net/2433/198617
DOI(出版社版): 10.1039/c4ob01953a
PubMed ID: 25420542
出現コレクション:学術雑誌掲載論文等

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