Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Paolo Stabile"'
Autor:
Sara Rossi, Davide Tramarin, William Maton, Brigida Allieri, Francesca Campi, Pieter Westerduin, Gilles Laval, Jason W. B. Cooke, Zadeo Cimarosti, Paolo Stabile, Nicola Giubellina
Publikováno v:
Organic Process Research & Development. 16:1598-1606
The studies carried out to develop a robust crystallization method for the substituted piperazinyl-quinoline (1) a compound potentially active in the treatment of depression, are described in this contribution. These studies include the control of a
Autor:
Sara Rossi, Paolo Stabile, Jason W. B. Cooke, Gilles Laval, Paola Russo, Roberta Pachera, Ramona Moretti, Pieter Westerduin, Zadeo Cimarosti, Nicola Giubellina, Francesco Tinazzi, William Maton
Publikováno v:
Organic Process Research & Development. 15:1287-1296
1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone, 1, was identified as a potential drug for the treatment of depression and anxiety. Herein is described the work carried out to select the manufacturing route and the pr
Autor:
Paolo Stabile, Giuseppe Guercio, Damiano Castoldi, Ornella Curcuruto, Arianna Ribecai, Alessandro Lamonica
Publikováno v:
Tetrahedron Letters. 51:4801-4805
A mild, general, convenient, and efficient one-pot synthesis of 2-phenyl-5-substituted-1,3,4-oxadiazoles is described. Both (hetero)aryl and alkyl carboxylic acids were efficiently condensed with benzohydrazide in the presence of TBTU to give diacylh
Autor:
William Maton, Fernando Bravo, Paolo Stabile, Daniele Andreotti, Arnaldo Nalin, Simone Spada, Roberto Profeta, Alcide Perboni, Federica Stazi, Damiano Castoldi, Anna Mingardi, Stefano Provera, Emanuele Miserazzi, Nicola Giubellina, Mario Mattioli, Roberta Pachera, Pieter Westerduin, Arianna Ribecai, Simon M. Bryant, Lucilla Turco, Angelo M. Manzo
Publikováno v:
Organic Process Research & Development. 14:1239-1247
An efficient scalable route to synthesize the enantiomerically pure tert-butyl-(1R,4S,6R)-4-(hydroxymethyl)-3-azabicyclo[4.1.0]heptane-3-carboxylate is described. Compared to the original routes, significant improvements were made by using an innovat
Autor:
Paolo Stabile, Arianna Ribecai, Nicola Giubellina, Sara Rossi, Giuseppe Guercio, Lucilla Turco, Claudio Bismara, Riet Dams, Pieter Westerduin, Damiano Castoldi, Alessandro Lamonica, Anna Nicoletti, Stefano Provera
Publikováno v:
Organic Process Research & Development. 14:1153-1161
The family of phosphodiesterase (PDE) enzymes hydrolyse cyclic nucleotides, cAMP and cGMP, leading to their inactivation as intracellular second messengers. Inhibition of these enzymes leads to an elevation of levels of cyclic nucleotides in the cell
Autor:
Angelo M. Manzo, Arianna Ribecai, Stefano Provera, Sara Rossi, Monica Delpogetto, Simone Guelfi, Pieter Westerduin, Marie Hourdin, Alcide Perboni, Sergio Bacchi, Lucilla Turco, Paolo Stabile
Publikováno v:
Organic Process Research & Development. 14:895-901
A case study on the synthesis of novel CRF-1 antagonists containing the 2,3-dihydro-1H-pyrrolo[2,3-b]pyridine moiety is presented. The development of ever more efficient synthetic routes allowed th...
Autor:
Pieter Westerduin, Alcide Perboni, Zadeo Cimarosti, Gilles Laval, Paolo Stabile, Jason W. B. Cooke, Nicola Giubellina
Publikováno v:
Organic Process Research & Development. 14:859-867
The development and scale-up of an optimized synthesis for a novel drug candidate for depression and anxiety is presented. The updated synthesis represents a convergent and efficient four-stage app...
Autor:
Arianna Ribecai, Paolo Stabile, Alessandro Lamonica, Ornella Curcuruto, Giuseppe Guercio, Damiano Castoldi
Publikováno v:
Tetrahedron Letters. 51:3232-3235
A mild, general, convenient and practical methodology for the selective copper-mediated mono N-arylation of unprotected 2-imidazolidinone was developed. Strong electron-donating groups and free hydroxy and amino groups on the aryl iodide substrates w
Publikováno v:
Tetrahedron. 59:2067-2081
3-Aryl-4-iodoisocoumarins, which were readily and efficiently prepared by regioselective iodolactonization of methyl 2-ynylbenzoates or the corresponding carboxylic acids, were used as precursors either to 3-arylisocoumarins, including naturally-occu
Publikováno v:
Tetrahedron. 58:5023-5038
5-Iodo-2(2 H )-pyranone derivatives have been selectively synthesized by reaction of stereodefined methyl 2-en-4-ynoates with iodine in MeCN, CH 2 Cl 2 or C 6 H 6 at 20°C (Method C) or by treatment of these esters with ICl in CH 2 Cl 2 at 20°C (Met