N4-ALKOXYCARBONYL-5-FLUOROCYTOSIN DERIVATIVES, PREPARATION THEREOF AND ANTI-CANCER AGENT COMPOSITION CONTAINING THEM AS ACTIVE INGREDIENTS

摘要

PURPOSE: Provided are N4-alkoxycarbonyl-5-fluorocytosin derivatives of formula(1), a preparation thereof and a less toxic anti-cancer agent composition containing them as active ingredients. CONSTITUTION: The method of preparation of N4-alkoxycarbonyl-5-fluorocytosin derivatives of formula(1) comprises: obtaining the compound of formula(7) by reacting the compound of formula(8) with sodium methoxide; obtaining the compound of formula(6) by reacting the compound of formula(7) with acetonide; obtaining the compound of formula(5) by hydroborating the compound of formula(6); obtaining the compound of formula(3) by reacting the compound of formula(5) with the compound of formula(4) under the presence of a base; obtaining the compound of formula(2) by oxidizing the compound of formula(3); obtaining the compound of formula(1a) by oxidizing the compound of formula(2); and obtaining finally the compound of formula(1) by esterifying the compound of formula(2). The anti-cancer agent composition contains the compound of formula(1) or their pharmaceutically allowed salts or their solution. In formula (1), R1 is hydrogen, C1-C7 alkyl and alkenyl; R2 is an atom group or a protective group which is easily hydrolyzed or de-protected in vivo, preferably hydrogen or acetyl group; R3 is C1-C7 alkyl or alkenyl group.