PROCEDEU PENTRU PREPARAREA UNOR DERIVATI AI TIAZOLO-(5,4-D)-PIRIMIDINE

摘要

Title cpds. of formula (I): (where R1 is H, phenyl or lower alkyl and R2 and R3 are piperazino or 1,4-diazacyclohept-1-yl (opt. substd. in the 4-posn. by acyl, carbamoyl, benzyl, lower alkyl or lower hydroxyalkyl), or morpholino, hexahydro-1,4-oxazepin-4-yl, thiomorpholino, hexahydro-1,4-thiazepin-4-yl, 1-oxido or 1,1-dioxido-thiomorpholino or -hexahydro-1,4-thiazepin-4-yl, dialkanolamino or alkylenediamino, any of the heterocyclic residues being opt. C-substd. by 1 or 2 lower alkyl residues) and their salts are hypotensives and, esp. antithrombotic (thrombocyte aggregation inhibiting) agents. Cpds. (I) are prepd. by reacting corresponding compounds carrying a leaving group instead of one or both of the residues R2 and R3 with an amine H-R2 or HR3. Products contg. a thiomorpholino or hexahydro-1,4-thiazepin-4-yl group may be oxidized to the corresponding 1-oxido or 1,1-dioxide derivatives. 1-Oxido or 1, 1-dioxido groupings may be removed by reaction with a hydrohalic acid. In products contg. a free imino groups, this may be acylated.