A series of 21 substituted pyrazolo[3,4-d]pyrimidines-4-amines were studied by (1)H and (13)C NMR. The application of two-dimensional techniques, HMQC and HMBC, allowed the complete assignment of the spectra for all the compounds.

Inspired by the reported antiviral activity of pyrimidines and triazolopyrimidines, two series 2-anilinopyrimidines (5a-e) 1-aryl-[1,2,4]triazolo[4,3-a]pyrimidines (14a-k) were designed synthesized as potential agents. X-ray crystallographic study compounds (14d) (14k) confirmed structure desired isomer revealed coplanarity fused [1,2,4]triazolo[4,3-a]pyrimidine rings with aryl side group. DFT ...

A novel one-flask synthetic method was developed in which 5-aminopyrazoles were reacted with N,N-substituted amides in the presence of PBr₃. Hexamethyldisilazane was then added to perform heterocyclization to produce the corresponding pyrazolo[3,4-d]pyrimidines in suitable yields. These one-flask reactions thus involved Vilsmeier amidination, imination reactions, and the sequential intermolecul...

2-Amino-3-functionally substituted thiophene de­ rivatives are important intermediates to the phar­ maceutically important thieno[2,3-d]pyrimidines [2]. These thiophene derivatives were available from the procedures published by K. Gewald [3, 4] via either the reaction of a-methylene ketones with active methylene nitriles in presence of elementary sulphur of from a-mercaptoketones and active me...

The treatment of Human African trypanosomiasis remains a major unmet health need in sub-Saharan Africa. Approaches involving new molecular targets are important; pteridine reductase 1 (PTR1), an enzyme that reduces dihydrobiopterin in Trypanosoma spp., has been identified as a candidate target, and it has been shown previously that substituted pyrrolo[2,3-d]pyrimidines are inhibitors of PTR1 fr...

A new synthetic route leading to functionalized 1H-1,2,3-triazole-4-carbonitriles has been developed. set of 1-aryl-5-methyl-1H-1,2,3-triazole-4-carbonitriles was obtained in high yields from readily available starting 1H-1,2,3-triazole-4-carboxylic acids via several protocols. Synthesized were examined as promising precursors the simple and efficient method for preparation 2-triazol-4-yl-thien...