6533b85ffe1ef96bd12c196f

RESEARCH PRODUCT

Tumorhemmende Wirkstoffe, 12. Mitt. 2-Ureido-4(3H)-pyrimidinone

Alfred KreutzbergerHorst Schimmelpfennig

subject

chemistry.chemical_compoundchemistryAmideDrug DiscoveryPharmaceutical ScienceMedicinal chemistry

description

Aus der Kondensation von Guanidincarbonsaureamid (1) mit den β-Ketocarbonsaureestern 2a–h resultieren die 2-Ureido-4(3H)-pyrimidinone 3a–h. Die Ubertragbarkeit dieser Reaktionsweise auf cyclische Ketocarbonsaureester geht aus der zu 2-Ureido-5,6,7,8-tetrahydro-4(3 H)-chinazolon (3i) fuhrenden Kondensation von 1 mit 2-Oxocyclohexancarbonsaureethylester (2i) hervor. Besonders 3h vermag turmorhemmende Effekte auszulosen. Tumor Inhibitory Agents, XII: 2-Ureido-4(3H)-pyrimidinones The condensation of guanidinecarboxylic amide (1) with the β-ketocarboxylates 2a-h leads to the 2-ureido-4(3H)-pyrimidinones 3a–h. The applicability of this reactin to cyclic ketocarboxylates is demonstrated by the condensation of 1 with ethyl 2-oxocyclohexanecarboxylate (2i) which yields 2-ureido-5,6,7,8-tetrahydro-4(3H)-quinazolone(3i). Compound 3h exhibits tumor inhibitory activity.

https://doi.org/10.1002/ardp.19813140107