Synthesis of Tegafur by the Alkylation of 5-Fluorouracil under the Lewis Acid and Metal Salt-Free Conditions
A novel protocol for preparation of tegafur (a prodrug of 5-fluorouracil) is reported. The process involves the 1,8-diazabicycloundec-7-ene-mediated alkylation of 5-fluorouracil with 2-acetoxytetrahydrofuran at 90 °C, followed by treatment of the prepurified mixture of the alkylation products with aqueous ethanol at 70 °C. The yield of the two-step process is 72%.
Anti-cancer composition for delivering 5-fluorouracil
An anti-cancer composition comprising a 5-fluorouracil (including derivatives thereof) and uracil (or salt thereof), is disclosed, wherein the composition contains less than 0.1 mole of the 5-fluorouracil per mole of the uracil.
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(2008/06/13)
5-FLUOROURACIL DERIVATIVES. VI. ALKYLATION OF 5-FLUOROURACIL USING THE (OCTYLTHIO)CARBONYL GROUP AS A PROTECTING FUNCTION
N1- and N3-alkyl-5-fluorouracils are prepared in good yields by the alkylation of 5-fluorouracil protected by the (octylthio)carbonyl group.