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  • Inventor(s):
    Marvin J. Miller, Julia M. Dolence, Manuka Ghosh
    Patent Number:
    US 5783689 B2

    5’-O-Acyl-5-fluorouridines and 5’-O-acyl-5-sluorocytidines are prepared by the direct acylation of the 5’-hydroxyl group with amino acids under Mitsunobu conditions and the amino acyl derivatives are coupled with other amino acids or peptides to provide antibacterial and antifungal derivatives of the nucleosides. For example, 5-fluorouridine is acylated at the 5’-hydroxyl group with an amino protected L-valine and the acylation product is deprotected to provide 5’-O-(L-val…

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