Heterocyclic amplifiers of phleomycin. II. Thiazol-4'-ylpyrazines with phenyl substituents and strongly basic side chains

Abstract

The preparation of a series of 2'-substituted 2-(thiazol-4'-1)pyrazines by ring closure of chloro-methylpyrazin-2-yl (and 3-,5- and 6-phenylpyrazin-2-yl) ketones with ammonium dithiocarbamate, methyl dithiocarbamate and N-methylthiourea are described. Mercapto compounds were converted into dimethylaminoalkyl(thio) derivatives. As amplifiers of phleomycin, N,N-dimethyl-3-[4'- (pyrazin-2-yl)thiazol-2'-ylthio]propylamne and N,N-dimethyl-2-[4'-(3''-phenylpyrazin-2''-yl)thiazol-2'-yl]thioethylamine showed three star activity.