Parallel synthesis of 2-substituted 6-(5-oxo-1-phenylpyrrolidin-3-yl)pyrimidine-5-carboxamides |
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Authors: | Crček Bojana Baškovč Jernej Grošelj Uroš Kočar Drago Dahmann Georg Stanovnik Branko Svete Jurij |
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Affiliation: | Faculty of Chemistry and Chemical Technology, University of Ljubljana, A?ker?eva 5, P.O. Box 537, 1000 Ljubljana, Slovenia. |
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Abstract: | A library of 24 6-(5-oxo-1-phenylpyrrolidin-3-yl)pyrimidine-5-carboxamides 10{1,2; 1-12} was prepared by a parallel solution-phase approach. The synthesis comprises a five-step transformation of itaconic acid (11) into 1-methyl and 1-phenyl substituted 6-(5-oxo-1-phenylpyrrolidin-3-yl)pyrimidine-5-carboxylic acids 17{1,2} followed by parallel amidation of 17{1,2} with a series of 12 aliphatic amines 18{1-12} to afford the corresponding carboxamides 10 in good overall yields and in 80-100% purity. |
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