Kolesnikov O. Derivatives of a pyrimidinthiones, quinazolinethiones and pyrimido[5,4-d]pyrimidine synthesis, chemical transformation and biological activity

Less studied 4-amino-5-arylsulfonyl-1H-pyrimidinethiones-2 and 4-amino-5-(2-thienylsulfonyl)-1H-pyrimidinthiones-2 and products of their alkylation were synthesized. It has been found that for the synthesis of 4-aminoquinazoline-2-thiones derivatives interaction of 2-isothiocyanobenzonitriles with amines can be usedFormation of an 4-aminoquinazoline-2-thiones takes place under Dymrot's reaction conditions. For expansion of class of the got connections it was conducted them alkilation. For the final leading to of structure of the synthesized connections, direction of alkilations and possibility of passing regrouping of Dymrot's, X-ray analysis. For the rational synthesis of an 2,4,6,8-tetrasubstituted pyrimido[5,4-d]pyrimidines which are potential purine mimetics, subsequent nucleophilic substitution reactions of an 2,4,6,8-tetrasubstituted pyrimido[5,4-d]pyrimidines (TCPP) has been studied. According to the results of the pharmacological screening was observed that 4-amino-5-(2-thienylsulfofnyl)-1H-pyrimidinethione-2-N-o-tolylacetamide is com-parative non-toxic and possess high level analgesic and action on the CNS. This substance is recommended for the further pharmacological studying and project of an analytical and technical documentation for this substance has been developed.