Machoń Z, Jasztold-Howorko R
Farmaco Sci. 1985 Sep;40(9):695-700.
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.
1-苯甲酰基-2-氧代-4,6-二羟基氮杂环丁烷并-[3,2-d]嘧啶(III)与二乙醇胺反应生成酰胺(IV)。将后者与亚硫酰氯加热得到2-β-氯乙基-8-羟基-9-苯甲酰氨基-全氢吡嗪并[1,2-c]嘧啶-1,6-二酮(VI)。化合物(VI)与不同的胺反应得到相应的2-β-氨基取代衍生物(VII-XIII)。所得到的一些化合物显示出中枢活性。