Cyotostatisch wirksame 2'-3'-Didesoxy-3'-fluorpyrimidin-nucleoside

摘要

The compounds are of formula I: Thymine - and are prepared by heating the corresponding 3'-OH compound, e.g. the pyrimidine-O23'-cyclo-2'-desoxy-nucleoside, for 30-60 mins. at 60-100 degrees pref. 80-90 degrees in an organic solvent containing up to 20%, pref. 4-6% anhyde. HF, KFHF or NH4F, distilling and purifying the residue by crystn. or column chromatography. Instead of the 3'-OH compound the 3'-sulphonyl (pref. mesylated)-pyrimidine nucleoside may be used. The above thymine deriv. at a concn. of 3 x 10-5M produces 87% inhibition of Ehrlich ascites carcinoma cells in mice and 50% inhibition of DNA synthesis at 2 x 10-4M concn.