Synthesis of perhydropyrazino [1,2-c] pyrimidine derivatives.
The reaction of 1-benzoyl-2-oxo-4,6-dihydroxyazetino-[3,2-d] pyrimidine (III) with diethanolamine affords the amide (IV). Heating of the last with SOCl2 yields 2-beta-chloroethyl-8-hydroxy-9-benzoylamino-perhydropyrazino [1,2-c] pyrimidine-1,6-dione (VI). Reaction of compound (VI) with different amines gives the respective 2-beta-aminosubstituted derivatives (VII-XIII). Some of the obtained compounds showed central activity.
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002490:Central Nervous System / Q000187:drug effects; D011719:Pyrazines / Q000138:chemical synthesis* / Q000494:pharmacology; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000893:Anti-Inflammatory Agents; D011719:Pyrazines; D011744:Pyrimidinones