An original route has been found for the synthesis of [1,4]diazepino-quinazolones, a new ring system of heterocondensed quinazolones. These anthranilicacid-alanin-β-alanin cyclopeptide derivatives constitute a structural moiety of asperlicin, the first natural cholecystokinin antagonist alkaloid. These compounds are therefore potential CCK antagonists. The new compounds were prepared via condensation of 2-amino-alkyl-quinazolones, obtained from 2-alkyl-quinazolones by side-chain substitution, with 1,3-bifunctional-reagents. We studied the cyclisation process under basic, acidic and phase-transfer catalyzed conditions. The structures of the synthesized compounds were characterized by IR, UV and NMR spectroscopy.
|Number of pages||6|
|Journal||Acta pharmaceutica Hungarica|
|Publication status||Published - Jan 1 1995|
ASJC Scopus subject areas
- Pharmaceutical Science