摘要 |
5'-Deoxy-5-fluorocytidine(I) and -uridine and their acid addn. salts, useful as antitumor agents, were prepd. from 5-fluorocytidine and 5-fluorouridine, resp. Thus, 5-fluorocytidine was treated with Me2C(OMe)2, the 2',3'-protected nucleoside was iodinated with tri-Ph phosphite methiodide, and the resultant 5'-deoxy-5'-iodo deriv. was catalytically hydrogenated and then deprotected to give I. I at a dose of 400 mg/kg, i.p., inhibited the growth of Sarcoma 180 in mice by 95%.
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