109253-05-6Relevant articles and documents
Ligand-Enabled meta-Selective C-H Arylation of Nosyl-Protected Phenethylamines, Benzylamines, and 2-Aryl Anilines
Ding, Qiuping,Ye, Shengqing,Cheng, Guolin,Wang, Peng,Farmer, Marcus E.,Yu, Jin-Quan
, p. 417 - 425 (2017)
A Pd-catalyzed, meta-selective C-H arylation of nosyl-protected phenethylamines and benzylamines is disclosed using a combination of norbornene and pyridine-based ligands. Subjecting nosyl protected 2-aryl anilines to this protocol led to meta-C - H arylation at the remote aryl ring. A diverse range of aryl iodides are tolerated in this reaction, along with select heteroaryl iodides. Select aryl bromides bearing ortho-coordinating groups can also be utilized as effective coupling partners in this reaction. The use of pyridine ligands has allowed the palladium loading to be reduced to 2.5 mol %. Furthermore, a catalytic amount of 2-norbomene (20 mol %) to mediate this meta-C - H activation process is demonstrated for the first time. Utilization of a common protecting group as the directing group for meta-C-H activation of amines is an important feature of this reaction in terms of practical applications.
Inhibitors of potassium channels KV1.3 and IK-1 as immunosuppressants
Pegoraro, Stefano,Lang, Martin,Dreker, Tobias,Kraus, Juergen,Hamm, Svetlana,Meere, Cathal,Feurle, Juliane,Tasler, Stefan,Pruetting, Sylvia,Kuras, Zerrin,Visan, Violeta,Grissmer, Stephan
scheme or table, p. 2299 - 2304 (2010/03/03)
New structural classes of KV1.3 and IK-1 ion channel blockers have been identified based on a virtual high throughput screening approach using a homology model of KcsA. These compounds display inhibitory effects on T-cell and/or keratinocyte pr