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Studies on pyrazine derivatives. Part V. Synthesis and tuberculostatic activity of some 6- (beta-aminoethoxy) -pyrazine-2-carboxylic acids

Foks, H.; Janowiec, M.; Sienicka, J.

Polish Journal of Pharmacology and Pharmacy 28(3): 295-300

1976

ISSN/ISBN: 0301-0244
PMID: 951310
Document Number: 100703
In the reaction of 2-cyano-6-chloropyrazine with sodium .beta.-aminoethanolates a mixture of nitriles (1) and imidoesters (2) was formed in relation depending on the reaction conditions. Compounds 1 and 2 with H2S and triethylamine gave thioamides (3), which were converted into amides and amidoximes (5). Alkaline hydrolysis of the derivatives of 6-(.beta.-aminoethoxy)-pyrazine-2-carboxylic acid of type 1, 2, 3 and 5 gave 6-ethoxypyrazine-2-carboxylic acid. The highest antituberculous activity (62.5-125 .mu.g/cm3) was shown by 2 thioamides.

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