Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...
Patent
1996-08-08
1997-12-02
Gupta, Yogendra N.
Organic compounds -- part of the class 532-570 series
Organic compounds
Nitrogen attached directly or indirectly to the purine ring...
544330, C07D23948
Patent
active
056938004
ABSTRACT:
A novel pyrimidine derivative, N-(2-amino-4,6-dichloropyrimidine-5-yl)formamide for use, e.g., in the production of antiviral nucleotide derivatives, can be made by a process involving cyclyzing an aminomalonic ester with guanidine or its salt in the presence of a base to produce 2,5-diamino-4,6-dihydroxypyrimidine or its salt, chlorinating this product with a chlorinating agent in the presence of an amide to produce 4,6-dichloropyrimidine, and reacting the 4,6-dichloropyrimidine with an aqueous solution of a carboxylic acid to produce the N-(2-amino-4,6-dichloropyrimidine-5-yl)formamide. Novel also are 4,6-dichloropyrimidine, 4,6-dichloro-N'-(dimethylaminomethylene)pyrimidine-2,5-diamine, 4,6-dichloro-N'-(piperidine-1-ylmethylene)pyrimidine-2,5-diamine, and a process for making 2,5-diamino-4,6-dichloropyrimidine of the formula ##STR1##
REFERENCES:
patent: 5294710 (1994-03-01), Stucky et al.
M. Legraverend et al., "A New Route to 2,5-Diamino-4,6-dichloropyrimidine . . . ", Synthesis, vol. 7 (1990), pp. 587-589.
C. Temple, Jr. et al., "Preparation of . . . ", Journal of Organic Chemistry, vol. 40 (1975), pp. 3141-3142.
C. Temple, Jr. et al., "Preparation of . . . ", Chemical Abstracts, vol. 89 (1978), p. 591, Abstract No. 215347s.
Imwinkelried Rene
Stucky Gerhard
Gupta Yogendra N.
Lonza AG
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