Preparation of 2-amino-4-fluoropyrimidine derivatives

Details Preparation of 2-amino-4-fluoropyrimidine derivatives Preparation of 2-amino-4-fluoropyrimidine derivatives

1989-12-18

1991-04-30

Shen, Cecilia

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

Organic compounds

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

544321, C07D23947

Patent

active

050119273

ABSTRACT:
A process for the preparation of 2-amino-4-fluoropyrimidine derivatives of the general formula I ##STR1## (R.sup.1 hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or benzyl, it being possible for the aromatic rings to be substituted, and R.sup.2 one of the R.sup.1 radicals with the exception of hydrogen) by reaction of 2,4,6-trifluoropyrimidine in an aprotic polar organic solvent with an amine of the formula III to give the 2-aminodifluoropyrimidine derivative IVa mixed with the 4-aminodifluoropyrimidine derivative IVb, separation of IVa out of the resulting reaction mixture and subsequent reaction of IVa with an alcohol in the presence of a base at from 0.degree. to 180.degree. C. to give the 2-amino-4-fluoropyrimidine derivative I, by carrying out the reaction of 2,4,6,-trifluoropyrimidine II with the amine III at from -80.degree. C. to -15.degree. C., and reacting the 2-aminodifluoropyrimidine derivative IVa with the alcohol in the presence of an organic base to give the 2-amino-4-fluoropyrimidine derivative I.

REFERENCES:
Chemical Abstracts (I), 85:77134, 1976.
Chemical Abstracts (II), 80:59913, 1974.
Chemical Abstracts (III), 80:14409, 1974.
J. Med. Chem. 6, 688 ff, 1963.
J. Chem. Soc. 6, 1280 ff, 1970.
SU-A 547 447 (1975), no equivalent abstract in CA 86, 190 000.
Schwamborn et al., Chem. Abst. 105-2232n (1986).
Ito et al. Chem. Abst. 107-134323u (1987).

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