A facile method for synthesis of N-acyloxymethyl-5-fluorouracils, as a class of antitumor agents.

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Abstract
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.