Synthesis of 1,2,4-Triazine Derivatives as Biologically Active Compounds

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1. Palladium catalyzed cross-coupling reaction of 3- and 5-iodo-1,2,4-triazine (as-triazines) with monosubstituted acetylenes gave the corrsponding alkynyll- as-triazines. The reaction of alkynyl-as-triazines with piperidine followed by the hydrolysis of the resulting enamines gave the acylmethyl-as-triazins.2. Methyl-diphenyl-as-triazines were treated with chloine to give trichloro- methyl-as-triazines. On treatment with excess of triphenylphosphine, diphenyl-- as-triazinyl)methylenetriphenylphosphoranes were obtained. The condensation of phosphoranes with various aldehydes affored alkenyl-diphenyl-as-triazines.3. The 3-methylsulfonyl-as-trizaine reacted with ONC-nucleophiles to give 3-substituted as-triazines. Similary, 5-subsituted and 6-substituted as-triazines were synthesized.4. The all as-triazines synthesized here were evaluated for antifungal activity against Pyricularia oryzae by the disk method. Among them, a series of 3-alkyl- thio-5-aryl-as-triazines were found to have the most potent antifungal activity, and the protective effects were determined by the pot tests.5. A series of as-triazines were tested for inhibitry activity toward arachidonic acid-induced aggregation of rabbit blood platelets in vitro. The 5,6-diaryl- as-triazines were found to have a potent activity activity as blood platelet aggregation inhibitors.