Parkhomenko O. Uses of multicomponent and domino-reactions for synthesis of derivatives of 2-thioxo-2,3-dihydro[1,3]thiazoles

Investigation objects: three-component condensation of CH-acidic nitriles, organic isothiocyanates and sulphur. Purpose: research of three-component condensation of CH-acidic nitriles, organic isothiocyanates and sulphur while using bifunctional re-agents and introducing additional components to reactionary medium. Methods: The synthesys of 2-thioxo-2,3-dihydro[1,3] thiazole derivatives, development of combinatorial libraries technology based on the obtained compounds, computer prog-noses of biological activity of the combinatorial libraries and biological screening for anti-microbial activity of the obtained compounds. Has been established: Double heterocyclization with cyanoacetamides, sulphur and isothiocyanates using re-agents possessing double cyanomethylene-active function has been studied. It has been proved that these compounds are really easy-forming and the process accomplishment does not require extra conditions for activating the second cyanoacetamide cen-tre. It has been determined that 2-carbometh¬oxiphen¬yliso¬thio¬cya¬nate and its derivatives' joining the reaction entails a dom-ino-reaction with closure of the two heterocycles at once and excreting agents of 1-thi¬oxo¬[1,3]¬thiazolo¬[3,4-?]¬qui¬na¬zo¬li¬ne-5(4H)-one heterocyclic system which had not been described yet. Malononitrile condensation with isothiocyanates was per-formed followed by excretion of derivatives of 4,6-diamino-2-thioxo-1,2-dihydro-3,5-piridine¬carbo¬di¬nit¬rile. In case of 2-carbomethoxiphenylthiocyanate joining the reaction, thermal cyclization becomes possible with excreting an agent of 3-amino-6-oxo-1-thioxo-5,6-dihydro-1H-pirido[1,2-?]-quinazoline-2,4-dicarbonitrile hete¬ro¬cycle which had not been described yet. Synthesis of novel heterocyclic systems has been performed due to combining biofunctionalities possessed by de-rivatives of methylene-active and isothiocyanatic nature, and on account of introducing additional components to reactionary medium. Degree of application: The results obtained can be used for newcombinatorial libraries syntheses which can use in drug research and development.