Pyrimidine reactions. Part XVIII. The conversion of 4-methoxy-5-nitropyrimidine into 3-amino-4-nitropyrazole by hydrazine
M. E. C. BIFFIN, D. J. Brown, QN Porter
Abstract
M. E. C. BIFFIN, D. J. Brown, QN Porter
Abstract
4-Methoxy-5-nitropyrimidine reacts with ethanolic hydrazine hydrate below 0° to give 4-hydrazino-5-nitropyrimidine which is converted by an excess of hydrazine hydrate at 25° into 3-amino-4-nitropyrazole. The mechanism, unprecedented in transformations of pyrimidines into pyrazoles, is discussed.The nitropyrazoles undergo hydrogenation to ortho-diamines which condense with α-dicarbonyl compounds to give pyrazolo[3,4-b]pyrazine and appropriate derivatives. Assigned structures are consistent with the measured u.v., i.r., 1H n.m.r., and mass spectra, and with ionization constants.
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4-Methoxy-5-nitropyrimidine reacts with ethanolic hydrazine hydrate below 0° to give 4-hydrazino-5-nitropyrimidine which is converted by an excess of hydrazine hydrate at 25° into 3-amino-4-nitropyrazole. The mechanism, unprecedented in transformations of pyrimidines into pyrazoles, is discussed.The nitropyrazoles undergo hydrogenation to ortho-diamines which condense with α-dicarbonyl compounds to give pyrazolo[3,4-b]pyrazine and appropriate derivatives. Assigned structures are consistent with the measured u.v., i.r., 1H n.m.r., and mass spectra, and with ionization constants.
Key concepts: Hydrazine (antidepressant), Hydrate, Chemistry, Pyrimidine, Combinatorial chemistry, Organic chemistry, Medicinal chemistry, Stereochemistry