Search Results - "Castoldi, Damiano"

A Formal Total Synthesis of Eleutherobin Using the Ring-Closing Metathesis (RCM) Reaction of a Densely Functionalized Diene as the Key Step: Investigation of the Unusual Kinetically Controlled RCM Stereochemistry by Castoldi, Damiano, Caggiano, Lorenzo, Panigada, Laura, Sharon, Ofer, Costa, Anna M., Gennari, Cesare

“…Asymmetric oxyallylation reactions and ring‐closing metathesis have been used to synthesize compound 3, a key advanced intermediate used in the total synthesis…”
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Mild and convenient one-pot synthesis of 1,3,4-oxadiazoles by Stabile, Paolo, Lamonica, Alessandro, Ribecai, Arianna, Castoldi, Damiano, Guercio, Giuseppe, Curcuruto, Ornella

“…Condensation of carboxylic acids with benzohydrazide in the presence of TBTU afforded diacylhydrazine intermediates that underwent a smooth TsCl-mediated…”
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Correction to “Development of a Control Strategy for a Defluorinated Analogue in the Manufacturing Process of Casopitant Mesylate” by Bravo, Fernando, Cimarosti, Zadeo, Tinazzi, Francesco, Castoldi, Damiano, Stonestreet, Paul, Galgano, Annalisa, Westerduin, Pieter

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Natural products with taxol-like anti-tumor activity: Synthetic approaches to eleutherobin and dictyostatin by Gennari, Cesare, Castoldi, Damiano, Sharon, Ofer

“…Eleutherobin and dictyostatin are antimitotic compounds which exert their cytotoxic activity by a taxol-like mode of action, i.e., hypernucleating tubulin…”
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Application of the QbD Principles in the Development of the Casopitant Mesylate Manufacturing Process. Process Research Studies for the Definition of the Control Strategy of some Drug Substance-CQAs for Stages 2a, 2b, and 2c by Cimarosti, Zadeo, Bravo, Fernando, Castoldi, Damiano, Tinazzi, Francesco, Provera, Stefano, Perboni, Alcide, Papini, Damiano, Westerduin, Pieter

“…Casopitant was identified as a potent NK1 antagonist by GlaxoSmithKline (GSK). It was selected as part of a wide drug discovery programme within GSK for its…”
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Mild, convenient and versatile Cu-mediated synthesis of N-aryl-2-imidazolidinones by Stabile, Paolo, Lamonica, Alessandro, Ribecai, Arianna, Castoldi, Damiano, Guercio, Giuseppe, Curcuruto, Ornella

“…A mild, general, convenient and practical methodology for the selective copper-mediated mono N-arylation of unprotected 2-imidazolidinone was developed. Strong…”
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Development of a Control Strategy for a Defluorinated Analogue in the Manufacturing Process of Casopitant Mesylate by Bravo, Fernando, Cimarosti, Zadeo, Tinazzi, Francesco, Castoldi, Damiano, Stonestreet, Paul, Galgano, Annalisa, Westerduin, Pieter

“…Casopitant mesylate was identified as part of the search for drugs with activity on the Central Nervous System (CNS) by GlaxoSmithKline. During late-phase…”
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Development of a Dynamic Kinetic Resolution for the Isolation of an Intermediate in the Synthesis of Casopitant Mesylate: Application of QbD Principles in the Definition of the Parameter Ranges, Issues in the Scale-Up and Mitigation Strategies by Bravo, Fernando, Cimarosti, Zadeo, Tinazzi, Francesco, Smith, Gillian E, Castoldi, Damiano, Provera, Stefano, Westerduin, Pieter

“…Process development towards the improvement of the manufacturing process of casopitant mesylate (a drug developed by GlaxoSmithKline with activity on the…”
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A Formal Total Synthesis of Eleutherobin Through an Unprecedented Kinetically Controlled Ring-Closing-Metathesis Reaction of a Densely Functionalized Diene by Castoldi, Damiano, Caggiano, Lorenzo, Panigada, Laura, Sharon, Ofer, Costa, Anna M., Gennari, Cesare

“…The key step in a formal total synthesis of eleutherobin was an unprecedented kinetically controlled RCM reaction of a densely functionalized diene 1 bearing…”
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Detection, identification and quantification of a new de-fluorinated impurity in casopitant mesylate drug substance during late phase development: An analytical challenge involving a multidisciplinary approach by Turco, Lucilla, Provera, Stefano, Curcuruto, Ornella, Bernabè, Elena, Nicoletti, Anna, Martini, Luca, Castoldi, Damiano, Cimarosti, Zadeo, Papini, Damiano, Marchioro, Carla, Dams, Riet

“…During late phase development of the selective NK1 receptor antagonist casopitant mesylate, a de-fluorinated impurity was discovered and quantified by an…”
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Overall Synthesis of GSK356278: Quick Delivery of a PDE4 Inhibitor Using a Fit-for-Purpose Approach by Guercio, Giuseppe, Castoldi, Damiano, Giubellina, Nicola, Lamonica, Alessandro, Ribecai, Arianna, Stabile, Paolo, Westerduin, Pieter, Dams, Riet, Nicoletti, Anna, Rossi, Sara, Bismara, Claudio, Provera, Stefano, Turco, Lucilla

“…The family of phosphodiesterase (PDE) enzymes hydrolyse cyclic nucleotides, cAMP and cGMP, leading to their inactivation as intracellular second messengers…”
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Effects of allylic and homoallylic substituents on the ring closing metathesis reaction used to synthesise simplified eleuthesides by Caggiano, Lorenzo, Castoldi, Damiano, Beumer, Raphael, Bayón, Pau, Telser, Joachim, Gennari, Cesare

“…During the course of our synthetic studies towards simplified eleuthesides, we have found that p-methoxyphenyl (PMP) protected allylic alcohols are compatible…”
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Synthesis of novel, simplified, C-7 substituted eleutheside analogues with potent microtubule-stabilizing activity by Castoldi, Damiano, Caggiano, Lorenzo, Bayón, Pau, Costa, Anna M., Cappella, Paolo, Sharon, Ofer, Gennari, Cesare

“…The synthesis of a number of novel, simplified, C-7 substituted eleutheside analogues with potent tubulin-assembling and microtubule-stabilizing properties is…”
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An Efficient Scalable Route for the Synthesis of Enantiomerically Pure tert-Butyl-(1R,4S,6R)-4-(hydroxymethyl)-3-azabicyclo[4.1.0]heptane-3-carboxylate by Maton, William M, Stazi, Federica, Manzo, Angelo Maria, Pachera, Roberta, Ribecai, Arianna, Stabile, Paolo, Perboni, Alcide, Giubellina, Nicola, Bravo, Fernando, Castoldi, Damiano, Provera, Stefano, Turco, Lucilla, Bryant, Simon, Westerduin, Pieter, Profeta, Roberto, Nalin, Arnaldo, Miserazzi, Emanuele, Spada, Simone, Mingardi, Anna, Mattioli, Mario, Andreotti, Daniele

“…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…”
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A Formal Total Synthesis of Eleutherobin Through an Unprecedented Kinetically Controlled Ring-Closing-Metathesis Reaction of a Densely Functionalized Diene by Castoldi, Damiano, Caggiano, Lorenzo, Panigada, Laura, Sharon, Ofer, Costa, Anna M., Gennari, Cesare

“…Der Schlüsselschritt in einer formalen Totalsynthese von Eleutherobin war die bisher unbekannte kinetisch kontrollierte RCM‐Reaktion des hochfunktionalisierten…”
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