Antitumor-active derivatives of 5-fluorouracil were prepared via a new method by introducing an acyloxymethyl group at the 1-, 3-, or 1, 3-position (s). These derivatives were obtained by condensing 1, 3-bis (hydroxymethyl) -5-fluorouracil with various short-/long-chain carboxylic acids or their derivatives, in the presence of dicyclohexylcarbodiimide and a catalytic amount of N, N-dimethylaminopyridine. Some of the derivatives showed strong antitumor activity against the leukemia L1210 system when administered orally.
A Facile Method for Synthesis of N-Acyloxymethyl-5-fluorouracils, as a Class of Antitumor Agents
SUHAIL AHMAD, SHOICHIRO OZAKI, AKIO HOSHI
Ehime University
National Cancer Center Research Institute
Chemical and Pharmaceutical Bulletin
1987 年
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