433958-64-6

Upstream product

• 71730-46-6 benzo[e][1,2,3]oxathiazine 2,2-dioxide 
• 120131-35-3 2-[1-(3-nitrophenyl)ethylidene]-malononitrile 
• 712350-28-2 N-[3-cyano-6-(2-hydroxyphenyl)-4-(3-nitrophenyl)-2-pyridinyl]thiophene-2-carboxamide 
• 433958-47-5 2-amino-6-(2-{[tert-butyl(dimethyl)silyl]oxy}-phenyl)-4-(3-nitrophenyl)pyridine-3-carbonitrile 
• 120820-40-8 1-(2-(((1,1-dimethylethyl)dimethylsilyl)oxy)phenyl)ethanone 
• 99-61-6 3-nitro-benzaldehyde 
• 433958-46-4 2-amino-4-(3-aminophenyl)-6-(2-{[tert-butyl(dimethyl)silyl]oxy}phenyl)nicotinonitrile 

Relevant academic research and scientific papers

Cu(OAc)2/DABCO-mediated domino reaction of vinyl malononitriles with cyclic sulfamidate imines: access to 6-hydroxyaryl-2-aminonicotinonitriles

A novel Cu(ii)–salt/DABCO-mediated one-pot access to a myriad of highly substituted biologically relevant 2-aminonicotinonitriles possessing a resourceful phenolic moiety with satisfactory yields is reported. This method involves cyclic sulfamidate imines as 1C1N sources and different kinds of acyclic/cyclic vinyl malononitriles as 4C sources for pyridine synthesis via a vinylogous Mannich-cycloaromatization sequence process, creating two new C–N bonds under mild conditions. Importantly, this de novo strategy is applicable to gram-scale syntheses, underlining the method's practicability and allowing for a wide range of substrates with excellent functional group tolerance.

SUBSTITUTED 4-ARYL PYRIDINES USED AS KISS-1 ANTAGONISTS

The invention relates to novel 4-aryl pyridines of formula (I), in which R1- R4 are defined as cited in claim 1, to methods for producing the same and to the use of said pyridines for the treatment and/or prophylaxis of diseases, in addition to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular painful conditions and/or urological dysfunction.

Discovery of novel and selective IKK-β serine-threonine protein kinase inhibitors. Part 1

IκB kinase β (IKK-β) is a serine-threonine protein kinase critically involved in the activation of the transcription factor Nuclear Factor kappa B (NF-κB) in response to various inflammatory stimuli. We have identified a small molecule inhibitor of IKK-β. Optimization of the lead compound resulted in improvements in both in vitro and in vivo potency, and provided IKK-β inhibitors exhibiting potent activity in an acute cytokine release model (LPS-induced TNFα).