Jones, James Holden published the artcilePyrazine diuretics. IV. N-Amidino-3-amino-6-substituted pyrazinecarboxamides, Related Products of pyrazines, the main research area is PYRAZINECARBOXAMIDES; DIURETICS; SALURETICS.
cf. CA 67: 100105q. The synthesis of a series of N-amidino-3-amino-6-substituted pyrazinecarboxamides (I) (R = MeS, MeSO2, PhCH2S, and Me2N) is described. Since more direct synthetic routes were unsuccessful, the intermediate 3-amino-6-substituted pyrazinecarboxylic acids were synthesized by nucleophilic displacement of the Cl from 6-chloro-4(3H)-pteridinones or their 3-methyl derivatives, followed by alk. hydrolysis. These were cyclized to the 2-methyl-6-substituted 4H-pyrazino[2,3-d][1,3]oxazin-4-ones, which upon reaction with a guanidine followed by hydrolysis, afforded the desired compounds When the N-amidino-3-amino-6-substituted pyrazinecarboxamides were assayed for saluretic and diuretic activity in normal rats, the 6-methylthio and the 6-benzylthio derivatives proved to be the most potent, while in the corresponding 3-acetamido series, the outstanding members were the 6-methylthio and the 6-methoxy derivatives
Journal of Medicinal Chemistry published new progress about Diuretics. 1125-56-0 belongs to class pyrazines, name is 3-Amino-6-chloropyrazine-2-carboxamide, and the molecular formula is C5H5ClN4O, Related Products of pyrazines.