PRODUCTION OF 3',5'-DISUBSTITUTED-2'-DEOXY-5-FLUOROURIDINE COMPOUND

摘要

PURPOSE:To produce the titled compound useful as a carcinostatic agent, economically, in an industrial scale, without using harmful fluorine gas, by reacting 3,5-disubstituted-2-deoxyribofuranosyl halide with a 5-fluoropyrimidine derivative in the presence of an organic acid. CONSTITUTION:The objective compound of formula III is produced by condensing the 3,5-disubstituted-2-deoxyribofuranosyl halide of formula I (R<1> is alcohol- protecting group; X is halogen) [e.g. 3,5-bis-O-(p-chlorobenzoyl)-2-deoxyribofuranosyl chloride] with the 5-fluoropyrimidine derivative of formula II (R<2> is organic silyl) [e.g. 5-fluoro-2,4-bis(trimethylsilyloxy)pyrimidine] in the presence of an organic acid (e.g. acetylacetone).