TH9441B - N4- (substrate-oxccarbonyl) -5-deoxyrid-5-fluorocidine - Google Patents

Abstract

Substances represented by the general formula (I) (chemical formula) (I), where R1 is a saturated straight-chain or branched hydrocarbon radical. or not saturated [where the number of carbon atoms in the longest straight chain of this hydrocarbon radical ranges from three to seven] or a radical with the formula -(CH2)nY [where n- is an integer from 0 to 4, where Y is the radical. Hydrolhexyl, or n is an integer from 2 to 4 where Y is a lower alkoxy radical with 1 to 4 carbon atoms or a phenyl radical] and R2 is a hydrocarbon atom or a hydro- radical. Easily liquefied under physiological conditions including hydrates and salvates of compounds with generic formula (I), can be used to treat tumors. Substances can be prepared By reacting a substance with the general formula R1-OCOC1 with N4-insubstutted-5'-deoxy-5-fluo. rosididine with the formula I above, where R2 represents the protection group. and, if necessary, eliminating the custody group, drug patents.

Claims (7)

1. Substances represented by the general formula (chemical formula) (l), where R1 is N-propyl, N-butyl, N-pentyl, isopentyl, neopen. Tyl, 3,3-dimethyl butyl, N-hexyl, 2-ethyl butyl, phenyl ethyl And cyclohexyl methyl and R2 are hydrogen atoms or radicals that are easily hydrolyzed under Physiological state Including hydrates or salvates of substances with the general formula (I) 2. N4- (butoxycarbonyl) -5 \ '- deoxy-5-fluorocidine 3.5 \ '- Deoxy-5-Fluoro -N4- (pentyloxyccarbonyl) vididine 4. Substance 5 \ '- Deoxy - 5 - Fluoro - N4 - (Propoxy Carbonyl) Cytidine, 5 \' - Deoxy - 5 - Fluoro - N4 - (hexyloxercarbonyl) citidine, 5 \ '- deoxi - 5 - fluoro - N4 - (isopentyloxycarbonyl) Citidine, 5 \ '- Deoxy - 5 - Fluoro - N4 - (Neopentyloxercarbonyl) Cytidine, 5 \' - Deoxy - N5 - ((3,3 - dimethyl butoxi) carbonyl] - 5 - fluorocitidine, 5 \ '- Deoxy - N4 - [(2 - etylbutyl ) Oxccarbonyl] - 5 - fluorocitidine, N4 - [(cyclohexylmethoxy) carbonyl] - 5 \ '- deoxy - 5 - Fluorocitidine, 5 \ '- Deoxy - 5 - Fluoro - N4 - ((2 - Phenylethoxi) Carbonyl] citidine, 2 \', 3 \ '- Dai - 0 - Acetyl - 5 \' - Deoxy - 5 - Fluoro - N4 - (Propoxy Carbonyl) Cytidine, 2 \ ', 3 \ '- Dai - 0 - Acetyl - N4 - (Butoxy Carbonyl) - 5 \' - Deoxy - 5 - Fluorocytidine, 2 \ ', 3 \ '- Dai - 0 - Benzoyl - N4 - (Butoxy Carbonyl) - 5 \' - Deoxy - 5 - Fluorocytidine, 2 \ ', 3 \' - Dai - 0 - Acetyl - 5 \ '- Deoxy - 5 - Fluoro - N4 - (Pentyloxocarbonyl) citidine, 2 \', 3 \ '- Dai - 0 - Acetyl - 5 \' - Deor Cc - 5 - fluoro - N4 - (isopentyl oxccarbonyl) citidine, 2 \ ', 3 \' - di - 0 - acetyl - 5 \ '- Deoxy - 5 - Fluoro - N4 - (hexyloxercarbonyl) citidine, 2 \', 3 \ '- Dai - 0 - acetyl - 5 \ '- deoxy - N4 - ((2 - etylbutyl) oxccarbonyl] - 5 - fluorocitidine, 2 \', 3 \ '- di - 0 - acetil - N4 \ '- [(cyclohexylmethoxy) carbonyl] - 5 \' - Deoxy - 5 - fluorocytidine, 2 \ ' , 3 \ '- Dai - 0 - Acetyl - 5 \' - Deoxy - 5 - Fluoro - N4 - ((2 - Phenylethoxi) - Carbonyl cytidine , 5. The process for creating a substance according to any of the claims 1-4 consists of reacting the substance represented by the general formula (II) (chemical formula) (II), where R4 is a hydroxy protected radical. The substance is represented by the general formula (III), R1 OCOCI (III), where R1 is the same as defined above. And if necessary, eliminate protection radicals 6. Pharmaceutical components In particular for the treatment of characterized neoplasms by containing substances with generic formulations (I) pursuant to claim 1, or hydrates or salvates of generic formulas (l ) Is an active ingredient 7. Use of any substance according to claim 1 - 4 for the production of antimicrobial agents