114114-86-2Relevant academic research and scientific papers
Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia
Bartolomé-Nebreda, José Manuel,Delgado, Francisca,Martín-Martín, María Luz,Martínez-Viturro, Carlos M.,Pastor, Joaquín,Tong, Han Min,Iturrino, Laura,Macdonald, Gregor J.,Sanderson, Wendy,Megens, Anton,Langlois, Xavier,Somers, Marijke,Vanhoof, Greet,Conde-Ceide, Susana
, p. 4196 - 4212 (2014/06/09)
We report the discovery of a series of imidazo[1,2-a]pyrazine derivatives as novel inhibitors of phosphodiesterase 10A (PDE10A). In a high-throughput screening campaign we identified the imidazopyrazine derivative 1, a PDE10A inhibitor with limited select
Phosphane ligands with two binding sites of differing hardness for enantioselective Grignard cross coupling
Terfort, Andreas,Brunner, Henri
, p. 1467 - 1479 (2007/10/03)
A series of new, chiral phosphanes is presented, individual members of which were designed to serve as ligands in transition-metal mediated asymmetric Grignard cross coupling reactions. These ligands are characterized by a side chain containing one or two oxygen atoms with the capacity to act as binding sites for the incoming Grignard reagent. A number of structural parameters for the compounds was varied to learn about the reaction mechanism. Most of the ligands were tested in two cross coupling reactions, the formation of 3-phenylbut-1-ene and of 2,2′-dimethyl-1,1′-binaphthyl, respectively. Although both systems gave modest enantiomeric excesses it was not possible to make a comparison of their respective abilities.
