Nucleosides of 5-monofluoromethyluracil and 5-difluoromethylurac

Details Nucleosides of 5-monofluoromethyluracil and 5-difluoromethylurac Nucleosides of 5-monofluoromethyluracil and 5-difluoromethylurac

1985-10-16

1988-08-09

Brown, J. R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

536 23, A61K 3170, C07H 1906

Patent

active

047628235

ABSTRACT:
A method for synthesizing monofluoromethyl- and difluoromethyluracil nucleosides from the corresponding thymine nucleosides is developed. These compounds which contain a partially fluorinated methyl group at the C-5 position (a new class of nucleosides) are potential antiviral and/or anticancer agents. The major features of the preparative route involve bromination of suitably protected thymine nucleosides followed by fluoride treatment.

REFERENCES:
patent: 3870700 (1975-03-01), Kotick et al.
patent: 4140850 (1979-02-01), Wierenga
patent: 4210638 (1980-07-01), Greer
patent: 4334059 (1982-06-01), Ogilvie
patent: 4382925 (1983-05-01), deClercq et al.
patent: 4594339 (1986-06-01), Lopez et al.

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