1. Parallel synthesis of 2-substituted 6-(5-oxo-1-phenylpyrrolidin-3-yl)pyrimidine-5-carboxamides
- Author
-
Jernej Baškovč, Drago Kočar, Uroš Grošelj, Georg Dahmann, Bojana Črček, Jurij Svete, and Branko Stanovnik
- Subjects
Magnetic Resonance Spectroscopy ,derivati amina ,Pyrimidine ,pyrimidines ,Carboxylic Acids ,Pharmaceutical Science ,heterocikli ,parallel synthesis ,pirimidini ,Article ,Analytical Chemistry ,lcsh:QD241-441 ,chemistry.chemical_compound ,paralelna sinteza ,organske reakcije ,lcsh:Organic chemistry ,Drug Discovery ,Combinatorial Chemistry Techniques ,Itaconic acid ,Physical and Theoretical Chemistry ,2-(heteroaryl)ethylamines ,Amines ,karboksamidi ,struktura spojin ,organska kemija ,heterociklični sistemi ,Chemistry ,sinteze ,Organic Chemistry ,Succinates ,NMR spektri ,Combinatorial chemistry ,Amides ,Pyrimidines ,derivati pirimidina ,udc:547.853.022.057 ,Chemistry (miscellaneous) ,2-(heteroaril)etilamini ,heterociklične spojine ,Molecular Medicine - 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.
- Published
- 2021