1153574-57-2Relevant articles and documents
Iridium-Catalyzed Asymmetric Hydrogenation of Unsaturated Piperazin-2-ones
Wang, Yanzhao,Liu, Yuanyuan,Li, Kun,Yang, Guoqiang,Zhang, Wanbin
, p. 1933 - 1941 (2017/06/09)
Two different iridium catalyst systems, generated from the ruthenocene-based phosphine-oxazoline ligand tBu-mono-RuPHOX or the diphosphine ligand BINAP, were developed for the asymmetric hydrogenation of 5,6-dihydropyrazin-2(1H)-ones, affording chiral piperazin-2-ones in good yields and with moderate to good ees. Different catalytic behaviors for the hydrogenation of these types of substrate were observed with these two catalyst systems. Our tBu-mono-RuPHOX ligand, which bears a ruthenocene scaffold with planar chirality, was found to be the best ligand for the [Ir(L)(COD)]BArF catalyst system, affording the desired products with up to 94% ee. (Figure presented.).
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis- trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor
Di Fabio, Romano,Griffante, Cristiana,Alvaro, Giuseppe,Pentassuglia, Giorgio,Pizzi, Domenica A.,Donati, Daniele,Rossi, Tino,Guercio, Giuseppe,Mattioli, Mario,Cimarosti, Zadeo,Marchioro, Carla,Provera, Stefano,Zonzini, Laura,Montanari, Dino,Melotto, Sergio,Gerrard, Philip A.,Trist, David G.,Ratti, Emiliangelo,Corsi, Mauro
experimental part, p. 3238 - 3247 (2010/04/03)
In an effort to discover novel druglike NK1 receptor antagonists a new series of suitably substituted C-phenylpiperazine derivatives was identified by an appropriate chemical exploration of related N-phenylpiperazine analogues, with the specifi