1343422-17-2Relevant academic research and scientific papers
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.
