FLUOROMETHYLTHIORIBOSE DERIVATIVE AND TUMOR TREATING AGENT

摘要

NEW MATERIAL:A compound expressed by formula I (R is -CF2H or -CFH2; R' is nucleic acid base). EXAMPLE:5'-Deoxy-5'-difluoromethylthioribofuranosyladenine. USE:A tumor treating agent. PREPARATION:A compound expressed by formula II is brought into contact with acetic anhydride in, e.g. pyridine, to provide 1, 2,3-tri-O-acetyl- fluoromethylthioribose expressed by formula III, which is then brought into contact with a hydrogen halide in an organic solvent and converted into an acylhalogenosaccharide expressed by formula IV. The resultant compound is subsequently condensed with a nucleic acid base to afford a compound expressed by formula V. Protecting groups of OH groups at the 2- and 3-positions of the ribose in the compound and protecting groups of the nucleic acid base part are eliminated to provide the aimed compound expressed by formula I.