- A NEW ROUTE TO THE SYNTHESIS OF 5-FLUOROURACIL
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Starting from tetrafluoropyrimidine (1), selective fluorine/chlorine exchange reactions and selective hydrogenolysis of the chlorine substituents are described.Combination of these methods, together with a subsequent hydrolysis reaction, provides a new route to the synthesis of 5-fluorouracil via 4,6-dichloro-2,5-difluoropyrimidine and 4-chloro-2,5-difluoropyrimidine.
- Baasner, B.,Klauke, E.
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p. 417 - 430
(2007/10/02)
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- Process for the selective hydrogenation of chlorine-containing pyrimidines and new pyrimidines
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Chlorine-containing pyrimidines are selectively hydrogenated with elimination of hydrogen chloride, without other substituents and/or the aromatic ring being significantly attacked, by using a hydrogenation catalyst and a hydrogen chloride acceptor. This process gives predominantly new pyrimidines.
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- Process for the preparation of 5-fluorocytosine
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5-fluorocytosine is prepared by reacting 2,5-difluoro-4-chloro-pyrimidine with a proton acid in the presence of water to yield 2-hydroxy-4-chloro-5-fluoropyrimidine and reacting the 2-hydroxy-4-chloro-5-fluoropyrimidine with ammonia to yield 5-fluoro-cytosine.
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