Synthesis of 4′-C-fluoromethylnucleosides as potential antineoplastic agents

✍ Scribed by Kenji Kitano; Shinji Miura; Hiroshi Ohrui; Hiroshi Meguro

• Publisher: Elsevier Science
• Year: 1997
• Tongue: French
• Weight: 478 KB
• Volume: 53
• Category: Article
• ISSN: 0040-4020
• DOI: 10.1016/s0040-4020(97)00844-2

✦ Synopsis

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-hydoxymethyI-D-ribofuranose, the key intermediate of 4'-C-methylnucleosides. Among these nucleosides, the 2'-deoxy derivative exhibited potent antineoplastic activity in vitro.