1343422-06-9Relevant academic research and scientific papers
Parallel synthesis of 2-substituted 6-(5-Oxo-1-phenylpyrrolidin-3-yl) pyrimidine-5-carboxamides
Crcek, Bojana,Baskovc, Jernej,Groselj, Uros,Kocar, Drago,Dahmann, Georg,Stanovnik, Branko,Svete, Jurij
, p. 5363 - 5384 (2012/09/07)
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.
Parallel synthesis of 1-substituted 5-(5-oxopyrrolidin-3-yl)-1 H -pyrazole-4-carboxamides
Perdih, Peter,Baskovc, Jernej,Dahmann, Georg,Groselj, Uros,Koar, Drago,Novak, Ana,Stanovnik, Branko,Svete, Jurij
, p. 2822 - 2832 (2011/10/09)
A parallel solution-phase synthesis of 5-(5-oxo-1-phenylpyrrolidin-3-yl)- 1H-pyrazole-4-carboxamide derivatives as conformationally constrained pyrazole analogues of histamine starting from itaconic acid was developed. The synthetic method comprises a five-step preparation of 1-substituted 5-(5-oxo-1- phenylpyrrolidin-3-yl)-1H-pyrazole-4-carboxylic acids followed by parallel amidation with various primary and secondary amines to give a library of 24 histamine analogues in good overall yields and in very high purities. The method is general and substrate-independent. All the amidations proceed smoothly and no major difference in reactivity is observed with respect to the structures of the reactants. Georg Thieme Verlag Stuttgart, New York.
