951883-98-0Relevant academic research and scientific papers
Palladium-catalysed dehydrogenative sp3 C-H bonds functionalisation into alkenes: A direct access to N-alkenylbenzenesulfonamides
Bheeter, Charles B.,Jin, Rongwei,Bera, Jitendra K.,Dixneuf, Pierre H.,Doucet, Henri
, p. 119 - 124 (2014/03/21)
The palladium-catalysed dehydrogenation of sp3 carbon-hydrogen bonds of N-alkylbenzenesulfonamides allows a simple access to N-alkenylbenzenesulfonamides. The reaction proceeds with easily accessible catalysts, with pivalate as a base, and allo
Design and discovery of a selective small molecule κ opioid antagonist (2-methyl- n -((2′-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl) methyl)propan-1-amine, PF-4455242)
Verhoest, Patrick R.,Sawant Basak, Aarti,Parikh, Vinod,Hayward, Matthew,Kauffman, Gregory W.,Paradis, Vanessa,McHardy, Stanton F.,McLean, Stafford,Grimwood, Sarah,Schmidt, Anne W.,Vanase-Frawley, Michelle,Freeman, Jodi,Van Deusen, Jeffrey,Cox, Loretta,Wong, Diane,Liras, Spiros
experimental part, p. 5868 - 5877 (2011/10/08)
By use of parallel chemistry coupled with physicochemical property design, a series of selective κ opioid antagonists have been discovered. The parallel chemistry strategy utilized key monomer building blocks to rapidly expand the desired SAR space. The potency and selectivity of the in vitro κ antagonism were confirmed in the tail-flick analgesia model. This model was used to build an exposure-response relationship between the ? Ki and the free brain drug levels. This strategy identified 2-methyl-N-((2′- (pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242, which entered phase 1 clinical testing and has demonstrated target engagement in healthy volunteers.
