Process for the preparation of 5-fluorocytosine

Details Process for the preparation of 5-fluorocytosine Process for the preparation of 5-fluorocytosine

1985-10-23

1987-10-27

Daus, Donald G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

C07D23930

Patent

active

047031212

ABSTRACT:
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.

REFERENCES:
patent: 2945038 (1960-07-01), Duschinsky et al.
patent: 3846429 (1974-11-01), Giller et al.
patent: 3954758 (1976-05-01), Schuman et al.
patent: 4113949 (1978-09-01), Schuman et al.
patent: 4473691 (1984-09-01), Takahara
Robert Filler and S. M. Naqvi in "Biomedical Aspects of Fluorine Chemistry", Eds. R. Filler and Y. Kobayashi, Elsevier, Amsterdam-New York-Oxford (1982).
J. Am. Chem. Soc., 79, 4559 (1957).
Kjell Undheim and Michel Gacek in "Some Derivatives of 5-Fluoropyrimidine", Chemical Institute University of Oslo, Acta Chem. Scand., 23, 294 (1969).

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