701977-09-5Relevant articles and documents
New efficient asymmetric synthesis of taranabant, a CB1R inverse agonist for the treatment of obesity
Crump, Brian R.,Phenix, Brian D.,Spindler, Felix,Wallace, Debra J.,Campos, Kevin R.,Shultz, C. Scott,Klapars, Artis,Zewge, Daniel,McWilliams, J. Christopher,Krska, Shane,Sun, Yongkui,Chen, Cheng-Yi
experimental part, p. 84 - 90 (2010/04/22)
Taranabant (1) is a cannabinoid-1 receptor (CB1R) inverse agonist that was recently in late-stage clinical development for the treatment of obesity. The previously employed synthesis exhibited a number of shortcomings for continuing development, and in th
Catalytic, enantioselective synthesis of taranabant, a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity
Chen, G-Yi,Frey, Lisa F.,Shultz, Scott,Wallace, Debra J.,Marcantonio, Karen,Payack, Joeseph F.,Vazquez, Enrique,Springfield, Shawn A.,Zhou, George,Liu, Ping,Kieczykowski, Gerard R.,Chen, Alex M.,Phenix, Brian D.,Singh, Utpal,Strine, Jeff,Izzo, Brianne,Krska, Shane W.
, p. 616 - 623 (2012/12/31)
Chiral amide 1 (MK-0364, taranabant) is a potent, selective, and orally bioavailable cannabinoid-1 receptor (CB-1R) inverse agonist indicated for the treatment of obesity. An asymmetric synthesis featuring a dynamic kinetic resolution via hydrogenation fo
FORMATION OF TETRA-SUBSTITUTED ENAMIDES AND STEREOSELECTIVE REDUCTION THEREOF
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Page/Page column 18; 32, (2008/06/13)
The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compo