928656-94-4

Upstream product

• 76-09-5 2,3-dimethyl-2,3-butane diol 
• 848649-38-7 4-bromobenzenesulfonic acid pentafluorophenyl ester 
• 73183-34-3 bis(pinacol)diborane 
• 98-58-8 4-bromobenzenesulfonyl chloride 

Downstream Products

• 928656-95-5 pentafluorophenyl 6'-amino-5'-(aminocarbonyl)-1,1':3',1''-terphenyl-4-sulfonate 
• 1160931-29-2 C₁₅H₂₄BNO₅S 
• 943434-47-7 N-(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzenesulfonamide 
• 1375457-32-1 perfluorophenyl 4-(5-methyl-2-(1-methyl-1H-pyrazol-4-ylamino)pyrimidin-4-yl)benzenesulfonate 
• 1375455-82-5 5-methyl-N-(1-methyl-1H-pyrazol-4-yl)-4-(4-(morpholinosulfonyl)phenyl)pyrimidin-2-amine 
• 1187448-98-1 1,1-dimethylethyl {2-[({4-[2-(1,1-dimethylethyl)-5-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl]phenyl}sulfonyl)amino]ethyl}carbamate 
• 1187449-25-7 1,1-dimethylethyl [2-({[4-(5-chloro-2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]sulfonyl}amino)ethyl]carbamate 
• 1014613-60-5 C₂₂H₃₅BN₂O₆S 
• 943434-46-6 N-(1,1-dioxidotetrahydro-3-thienyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzenesulfonamide 
• 1014613-14-9 1,1-dimethylethyl [2-({[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]sulfonyl}amino)ethyl]carbamate 

Relevant academic research and scientific papers

Syntheses of (4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)arenes through Pd-catalyzed borylation of arylbromides with the successive use of 2,2′-bis(1,3,2-benzodioxaborole) and pinacol

Syntheses of (4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)arenes through the Pd-catalyzed borylation of arylbromides with the successive use of 2,2′-bis(1,3,2-benzodioxaborole) and pinacol were investigated. PdCl 2(dppf) and AcOK in EtOH or DMSO successfully provided (4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)arenes. In particular, this method was more effective in the borylation of arylbromides bearing sulfonyl groups than the conventional Pd-catalyzed borylation using pinacolborane or bis(pinacolato)diboron.

PYRIDINE COMPOUNDS AND AZA ANALOGUES THEREOF AS TYK2 INHIBITORS

The present invention relates to compounds of formula (I), wherein R1 to R3, X1, X2 have the meaning as cited in the description and the claims. Said compounds are useful as TYK2 inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds as well as their use as medicaments.

4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors

The synthesis and SAR of a novel series of IKK2 inhibitors are described. Modification around the hinge binding region of the 7-azaindole led to a series of potent and selective inhibitors with good cellular activity.

O-HYDROXY- AND O-AMINO BENZAMIDE DERIVATIVES AS IKK2 INHIBITORS

A compound of Formula (I).