Fluorocytidine derivatives

Details Fluorocytidine derivatives Fluorocytidine derivatives

1988-11-08

1990-10-30

Shen, Cecilia

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

536 23, C07H 1906, A61K 31505

Patent

active

049668919

ABSTRACT:
The novel 5'-deoxy-5-fluorocytidine derivatives of formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are hydrogen or an easily hydrolyzable radical under physiological conditions, with the proviso that, at least one or R.sup.1, R.sup.2 and R.sup.3 is an easily hydrolyzable radical under physiological conditions,
as well as hydrates of solvates of these compounds have antitumor properties. They can be prepared from compounds of formula I, wherein R.sup.1 is hydrogen or an amino-protecting radical and R.sup.2 and R.sup.3 are hydrogen or a hydroxy-protecting radical or taken together are a cyclic hydroxy-protecting radical.

REFERENCES:
patent: 3404144 (1968-10-01), Fox et al.
patent: 4071680 (1978-01-01), Cook
patent: 4122251 (1978-10-01), Misaki et al.
patent: 4659698 (1987-04-01), Imbach et al.
patent: 4816569 (1989-03-01), Miyoshi
Briggle et al., Chem. Abs. 105:218184w (1986).
Cook et al., Journal of Medicinal Chem. vol. 22, 1330-6, (1979) "Fluorinated Pyrimidine Nucleosides . . . ".
Matsuda et al., Chem. Pharm. Bull. 33(6) 2575-2578, (1985) "Reaction of Uracil Nucleosides with . . . ".

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