Suzuki coupling reaction for the solid-phase preparation of 5-substituted nicotinic acid derivatives
The application of the Suzuki coupling reaction to the preparation of small combinatorial libraries using 5-bromonicotinic acid as a scaffold onto three different types of solid support (Wang, Rink, and BAL resin) is described. The application of the Suzuki coupling reaction to the preparation of small combinatorial libraries using 5-bromonicotinic acid as a scaffold onto three different types of solid support (Wang, Rink, and BAL resin) is described.
Fernàndez, Joan-Carles,Solé-Feu, Laia,Fernández-Forner, Dolors,De La Figuera, Natalia,Forns, Pilar,Albericio, Fernando
Subtype-selective Nav1.8 sodium channel blockers: Identification of potent, orally active nicotinamide derivatives
A series of aryl-substituted nicotinamide derivatives with selective inhibitory activity against the Nav1.8 sodium channel is reported. Replacement of the furan nucleus and homologation of the anilide linker in subtype-selective blocker A-803467 (1) provided potent, selective derivatives with improved aqueous solubility and oral bioavailability. Representative compounds from this series displayed efficacy in rat models of inflammatory and neuropathic pain.
Kort, Michael E.,Atkinson, Robert N.,Thomas, James B.,Drizin, Irene,Johnson, Matthew S.,Secrest, Matthew A.,Gregg, Robert J.,Scanio, Marc J.C.,Shi, Lei,Hakeem, Ahmed H.,Matulenko, Mark A.,Chapman, Mark L.,Krambis, Michael J.,Liu, Dong,Shieh, Char-Chang,Zhang, Xufeng,Simler, Gricelda,Mikusa, Joseph P.,Zhong, Chengmin,Joshi, Shailen,Honore, Prisca,Roeloffs, Rosemarie,Werness, Stephen,Antonio, Brett,Marsh, Kennan C.,Faltynek, Connie R.,Krafte, Douglas S.,Jarvis, Michael F.,Marron, Brian E.
scheme or table
p. 6812 - 6815
(2011/01/04)
METHOD FOR THE PRODUCTION OF NICOTINALDEHYDES
The invention relates to a method for producing nicotinaldehydes by reducing the corresponding nicotinic acid-morpholine amides.
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Page/Page column 9
(2008/06/13)
Method for producing 5-aryl nicotinaldehydes
The invention relates to a process for the preparation of 5-arylnicotinaldehydes by reduction of the corresponding 5-arylnicotinic acids by catalytic hydrogenation in the presence of carboxylic anhydrides in which the catalyst used is a palladium/ligand complex, characterized in that the molar ratio between palladium and ligand is from 1:5 to 1:15 in the case of monodentate ligands and from 1:2.5 to 1:7.5 in the case of bidentate ligands.
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(2008/06/13)
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