Patent ID: 6593467
Filing Date: 2003-07-15
Classification: C07H

Abstract:
A process for the preparation of 5â€²-deoxy-5-fluorouridine of formula I which comprises: a) reacting 2â€²,3â€²-O-isopropylidene-5-fluorouridine of formula II with a functional derivative of a sulfonic acid of formula III Râ€”SO3Hâ€ƒâ€ƒIII wherein R is a (C1-C4)alkyl, a trifluoromethyl, an unsubstituted, mono-di- or trisubstituted phenyl group; b) reacting the 5â€²-sulfonyloxyderivative thus obtained of formula IV wherein R is as defined above, with an alkaline or earth-alkaline iodide; c) hydrolyzing the 5â€²-deoxy-5â€²-iodo-2â€²,3â€²-O-isopropylidene-5-fluorouridine of formula V thus obtained in acidic medium; and d) submitting the 5â€²-deoxy-5â€²-iodo-5-fluorouridine of formula VI to a reduction with hydrogen or a hydrogen donor; wherein steps (a), (b) and (c) are carried out without isolating the products obtained at the end of each of the steps (a) and (b).