A Facile Method for Synthesis of N-Acyloxymethyl-5-fluorouracils, as a Class of Antitumor Agents

Abstract

Antitumor-active derivatives of 5-fluorouracil were prepared via a new method by introducing an acyloxymethyl group at the 1-, 3-, or l,3-position(s). These derivatives were obtained by condensing l,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. © 1987, The Pharmaceutical Society of Japan. All rights reserved.