Synthesis of 4′-C-Fluoromethylnucleosides as Potential Antineoplastic Agents

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• 作者：Kitano ; Kenji ; Miura ; Shinji ; Ohrui ; Hiroshi ; Meguro ; Hiroshi
• 刊名：Tetrahedron
• 出版年：1997
• 出版时间：September 29, 1997
• 年：1997
• 卷：53
• 期：39
• 页码：13315-13322
• 全文大小：491 K

文摘

2-Deoxy-d-erythro-, ribo-, and arabino-pentofuranosylcytosines, which have a fluoromethyl group at the 4′-position, were synthesized. Introduction of fluorine was achieved by DAST treatment of 4-C-hydroxymethyl-d-ribofuranose, the key intermediate of 4′-C-methylnucleosides. Among these nucleosides, the 2′-deoxy derivative exhibited potent antineoplastic activity in vitro.