Collect. Czech. Chem. Commun. 1982, 47, 2525-2529

2-Substituted derivatives of 5-(4-oxo-3,4-dihydro-5-pyrimidinyl)pentanoic acid

Rudolf Kotva, Jiří Křepelka and Jaroslav Vachek

Research Institute for Pharmacy and Biochemistry, 130 60 Prague 3


Condensation of trialkyl esters of 6-substituted 2-carboxy-1,7-heptanedioic acids XII-XVII with urea or thiourea and subsequent saponification gave 2-substituted 5-(2,6-dihydroxy-4-oxo-3,4-dihydro-5-pyrimidinyl)pentanoic acids II-VI or 5-(2-mercapto-6-hydroxy-4-oxo-3,4-dihydro-6-pyrimidinyl)pentanoic acids VII-XI, respectively. Compounds II, VII and X had a weak antineoplastic effect in animals with experimental transplantable tumours.