951883-94-6Relevant articles and documents
Structurally Diverse Synthesis of Five-, Six-, and Seven-Membered Benzosultams through Electrochemical Cyclization
Liu, Aiyun,Guo, Tiantian,Zhang, Shuangshuang,Yang, Han,Zhang, Qi,Chai, Yonghai,Zhang, Shengyong
supporting information, p. 6326 - 6331 (2021/08/23)
We have developed a metal- and oxidant-free approach to structurally diverse synthesis of benzosultams from aryl sulfonamides through an electrochemical cyclization. Upon variation of the ortho substituent on aryl sulfonamides, five-, six-, and seven-memb
Palladium-catalyzed C-C coupling of aryl halides with isocyanides: An alternative method for the stereoselective synthesis of (3E)-(Imino)isoindolin- 1-ones and (3E)-(imino)thiaisoindoline 1,1-dioxides
Liu, Bifu,Li, Yibiao,Jiang, Huanfeng,Yin, Meizhou,Huang, Huawen
, p. 2288 - 2300 (2012/11/07)
A palladium-catalyzed, one-pot cyclization reaction to construct (3E)-(imino)isoindolin-1-ones and (3E)-(imino)thiaisoindoline 1,1-dioxides by introducing ortho-reactive functional groups on aryl halides is reported. Under optimal conditions, the cyclization reaction afforded the corresponding products in good to excellent yields (up to 93%) with high stereoselectivity. Notably, this transformation successfully extends its application for the synthesis of phenanthridines and dibenzooxazepines. This new synthetic protocol not only extends the application platform for palladium-catalyzed C-C coupling of aryl halides with isocyanides, but also opens atom-economic and step-economic synthetic routes for nitrogen-containing heterocyclic compounds with wide functional group compatibility. Copyright
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.
PHENETHANOLAMINE DERIVATIVES FOR THE TREATMENT OF RESPIRATORY DISEASES
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Page 44-45, (2010/02/06)
The present invention relates to novel compounds of formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.