5-Fluorouracil derivatives. II. A convenient synthesis of 5-fluoro-2'-deoxyuridine.

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概要

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• The reaction of 5-fluorouridine with propionyl bromide in acetonitrile afforded 3′,5′-di-<I>O</I>-propionyl-2′-bromo-5-fluoro-2′-deoxyuridine (<B>2</B>). Compound <B>2</B> was then hydrogenated, using Pd–C as the catalyst, to afford 3′,5′-di-<I>O</I>-propionyl-5-fluoro-2′-deoxyuridine (<B>3</B>). Compound <B>3</B> was deacylated with methanolic ammonia to give 5-fluoro-2′-deoxyuridine (FUDR). In this way, FUDR, a good antitumor agent, can easily be prepared from 5-fluorouridine by three steps in a 48.9% total yield.

• 公益社団法人 日本化学会の論文

著者

• SANEYOSHI MINEO

  Faculty of Pharmaceutical Sciences, Hokkaido University

• Saneyoshi Mineo

  Faculty Of Pharmaceutical Sciences Hokkaido University

• Ozaki Shoichiro

  Research Center, Mitsui Toatsu Chemicals, Inc.

• Katakami Tsutomu

  Research Center, Mitsui Toatsu Chemicals, Inc.

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