Abstract
Unprecedented trisubstituted tetrahydropyrimidine-2,4-diones were easily synthesized in two steps involving Boc-amide protection and controlled ring opening, from perhydropyrazino[1,2-f ]pyrimidine-3,6,8-triones. These bicyclic derivatives were prepared by reaction of 2-oxopiperazines derived from dipeptides with isocyanates, followed by cyclization. The monocyclic pyrimidinone derivatives were further elaborated to potential CCK ligands that have contributed to a better understanding of the structural requirements for efficient binding at the CCK1 receptor.
Key words
heterocycles - peptides - bicyclic compounds - ring opening - medicinal chemistry
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