METHOD OF PREPARING N-ACYL-5'-DESOXY-5'-FLUOROCITIDINE DERIVATIVES Russian patent published in 1999 - IPC

FIELD: medicine. SUBSTANCE: N⁴-acyl-5'- desoxy-5-fluorocitidine derivatives of general formula (I): wherein R² is alkyl, cycloalkyl, alkenyl, alkoxyl, aralkyl such as benzyl, aryl such as phenyl optionally substituted by halogen atom, one to three alkoxy groups, nitro group, alkyl group; five-or six- membered heterocyclic residue such as furyl, thienyl, pyridyl using acylation reactions and removing protective groups, are valuable antitumor medicinals. 5- fluorocitozine is made to react with compound of general formula (II): wherein R¹ is lower alkyl or alkyl substituted phenyl, and Y is halogen atom, acycloxy or alkoxy group, the resulting compound of formula (III): wherein R¹ is as defined above, is acylated with respect to amino group, and the resulting compound of formula (IV): wherein R¹ and R² are as defined above, are subjected to deacylation to remove radicals R¹CO. Method is simple and easy to be carried out. EFFECT: more efficient preparation method. 5 cl, 49 ex, 5 tbl