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US 5,476,932 AGranted
Process for producing N4-acyl-5'-deoxy-5-fluorocytidine derivatives
AssigneeHoffmann-La Roche Inc.
InventorsHerbert R. Brinkman, Panayiotis Kalaritis, John F. Morrissey
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Abstract
A process for preparing N4-acyl-5'-deoxy-5-fluorocytidine derivatives of formula III: ##STR1## by selective deacylation, wherein R is alkyl, cycloalkyl, alkenyl, aralkyl or aryl, which comprises reacting a compound of formula II, ##STR2## wherein R is as defined above, with a base in an aqueous or inert organic solvent.
Claims5
A process for producing N4-acyl-5'-deoxy-5-fluorocytidine derivatives of formula III:
- ##STR9## wherein R is alkyl, cycloalkyl, alkenyl, aralkyl or aryl, which comprises treating a compound of formula II:
- ##STR10## wherein R is as above, in an aqueous or inert organic solvent, in a base selected from the group consisting of an alkali metal alkoxide, triethylamine, 1,8-diazabicyclo (5.4.0 undec-7-ene), N-methyl morpholine, pyridine, ammonium hydroxide and sodium hydroxide, to produce said fluorocytidine derivatives of formula III.
Dependencies are inferred from the claim text.