AMINATION OF 2-(2-OXO-2-ARYLETHYLTHIO)-PYRIMIDIN-4(3H)-ONE DERIVATIVES USING THE SULFONATE METHOD

A Derivatives of 2-thiouracil are characteri­zed by wide spectrum biological activity, which is characteristic most representatives this heterocycles class. In particular, 2-(2-oxo-2-phenylethylthio)-pyrimi­din-4(3H)-ones belong to the group non-nucleoside inhibitors HIV-1 reverse transcriptase. The antimalarial properties 2-(2-oxo-2-phenylethyl­thio)-4-R-pyrimidine derivatives, proved be effective CIpP protease Plasmodium falciparum, being studied. Known examples 2-(2-oxo-2-phenylethyl­thio)-pyrimidines modification at "4" position heterocycle limited use 4-chloro which, in turn, formed according classical method reaction pyrimidine-4(3H)-ones with POCl3 boiling point mixture. work, we present an alternative version above-mentioned class compounds. By amination amide function 6-R-2-(2-oxo-2-arylethylthio)-pyrimidin-4(3H)-ones derivati­ves ethanolamine and 1-aminopropa­ne-2,3-diol using sulfonate method, synthesized characterized new compounds a 6-R-2-(2-oxo-2-phenylethylthio)-pyrimidines series spectral methods. advantages scheme discussed (the formation intermediate sulfonates stage do not require harsh conditions carried out satisfactory yields). proposed can recommended cases where original substrate contains functio­nal groups that labile high temperatures sensitive acidic environment.