5'-DEOXY-N-ALKYLOXYCARBONYL-5-FLUOROCYTOSINE-5'-THIOESTER DERIVATIVES, PREPARATION METHOD THEREOF, ANTICANCER AGENT CONTAINING THE SAME AS EFFECTIVE COMPONENTS

摘要

PURPOSE: 5'-Deoxy-N-alkyloxycarbonyl-5-fluorocytosine-5'-thioester derivatives, a preparation method thereof, an anticancer agent containing the same as effective components are provided. The compounds have improved anticancer effect and low toxicity. CONSTITUTION: 5'-deoxy-N-alkyloxycarbonyl-5-fluorocytosine-5'-thioester derivatives are represented by the formula(1), wherein R1 is hydrogen, or C1-C10 saturated or unsaturated carbohydrate; R2 is hydrogen, or atom group easily hydrolyzed under physiological condition or easily removable protecting group; and R3 is C2-C7 saturated or unsaturated carbohydrate. A method for preparing the 5'-deoxy-N -alkyloxycarbonyl-5-fluorocytosine-5'-thioester derivatives of the formula(1) comprises the steps of: (a) reacting a compound of the formula(2) with thiol of the formula(3) of R1-SH in the presence of a solvent to prepare a compound of the formula(1b); and (b) deprotecting the compound of the formula 1b.