5-fluoro-2'-deoxyuridine derivative and its preparation

Abstract

Abstract NEW MATERIAL:The compound of formula I [A is 1-30C bivalent aliphatic hydrocarbon group; n is 0 or 1, when n is 0, Y is bonded directly to O; Y is H or (substituted) phenyl (when Y is h, n is 1 and A is unsaturated bivalent aliphatic group); R is H or alcohol-protecting group] and its salt. EXAMPLE:3'-Acetyl-5-fluoro-2'-deoxyuridine-5'-(9-cis-octadecenyl) phosphate. USE:Antitumor agent. PROCESS:The objective compound can be prepared by reacting the 3'-substituted- 5-fluoro-2'-deoxyuridine of formula II (R' is alcohol-protecting group) with the phosphoric acid monoester of formula III preferably in an aprotic organic solvent in the presence of a condensation agent (e.g. p-toluenesulfonyl chloride), and if necessary, removing the protecting group from the product.

Inventors

• 👤 Kenzo Watanabe
• 👤 兼三 渡辺
• 👤 Yoshinori Kato
• 👤 加藤　喜規
• 👤 Masahiko Saito
• 👤 斉藤　政彦
• 👤 Takeo Oba
• 👤 大場　丈夫
• 👤 Hisashi Fukushima
• 👤 福島　久
• 👤 Takeshi Hara
• 👤 健 原

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