877401-42-8

Basic information

• Product Name: tert-butyl 4-(4-(6-amino-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-3-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate
• Synonyms: tert-butyl 4-(4-(6-amino-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-3-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate
• CAS NO: 877401-42-8
• Molecular Weight: 550.46
• Mol File: 877401-42-8.mol
• Article Data: 6

Chemical Properties

• CAS DataBase Reference: tert-butyl 4-(4-(6-amino-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-3-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate(CAS DataBase Reference)
• NIST Chemistry Reference: tert-butyl 4-(4-(6-amino-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-3-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate(877401-42-8)
• EPA Substance Registry System: tert-butyl 4-(4-(6-amino-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-3-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate(877401-42-8)

Safety Data

• Hazardous Substances Data: 877401-42-8(Hazardous Substances Data)

Upstream product

• 756509-08-7 3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1H-pyrazol-4-yl)pyridin-2-amine 
• 141699-59-4 1-(tert-butoxycarbonyl)piperidin-4-yl methanesulfonate 
• 877399-08-1 (±)-3-(1-(2,6-dichloro-3-fluoropheny)ethoxy)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-amine 
• 877399-50-3 4-(4-bromo-1H-pyrazol-1-yl)piperidine-1-carboxylic acid tert-butyl ester 
• 756520-66-8 1-(2,6-dichloro-3-fluorophenyl)ethanol 
• 756521-08-1 (±)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-2-nitropyridine 
• 756520-67-9 (±)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-amine 
• 756503-69-2 (±)-5-bromo-3-(1-(2,6-dichloro-3-fluoropheny)ethoxy)pyridin-2-amine 
• 1331786-33-4 (±)-bis(Boc)-5-bromo-3-(1-(2,6-dichloro-3-fluoropheny)ethoxy)pyridin-2-amine 
• 1331786-34-5 (±)-bis(Boc)-3-(1-(2,6-dichloro-3-fluoropheny)ethoxy)-5-(4,4,5,5-tetramethyl-1 ,3,2-dioxaborolan-2-yl)pyridin-2-amine 
• 290835-85-7 2',6'-dichloro-3'-fluoroacetophenone 
• 877399-74-1 tert-butyl 4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate 
• 74115-13-2 5-bromopyridine-3-ol 
• 691872-15-8 5-bromo-3-hydroxy-2-nitropyridine 

Downstream Products

• 877400-66-3 (+/-)-PF023401066 
• 1428476-71-4 N-(3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(1-ethylpiperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-yl)acetamide 
• 1428476-72-5 3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-N-ethyl-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine 
• 1428476-85-0 tert-butyl 4-(4-(5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-6-(ethylamino)pyridin-3-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate 
• 1428476-87-2 tert-butyl 4-(4-(6-acetamido-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-3-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate 

Relevant articles and documents

Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2

Janus Kinase 2 (JAK2) is a kind of intracellular non-receptor protein tyrosine kinase and has been certified as an important target for the treatment of myeloproliferative neoplasms and rheumatoid arthritis. However, the low selectivity and potential safety issues restrict the clinical applications of JAK2 inhibitors. Here we found that crizotinib showed good inhibitory activity against JAK2 by enzymatic assays (IC50 = 27 nM). Then we carried out structure-based drug design and synthesized a series of compounds with an aminopyridine scaffold. Finally, compound 12k and 12l were identified as the promising inhibitors of JAK2, which exhibited high inhibitory activity (IC50 = 6 nM and 3 nM, respectively) and selectivity for JAK2 over JAK1 and JAK3, and showed potent antiproliferative activities toward HEL human erythroleukemia cells. Moreover, 12k suppressed symptoms of the collagen-induced arthritis (CIA) model in rats.

PYRIDINE COMPOUNDS AS INHIBITORS OF KINASE

Disclosed are pyridines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities and are expected to be useful for the treatment of protein kinases mediated diseases and conditions.

AMINOHETEROARYL COMPOUNDS AS FOR THE TREATMENT OF DISEASES MEDIATED BY C-MET KINASE ACTIVITY

Compounds of formula (I), are inhibitors of c-Met kinase activity, useful inter alia in the treatment of hyperproliferative diseases: wherein X is -N= or -CH=; ring A is optionally substituted mono- or bi-cyclic aryl or heteroaryl having from 5 to 12 ring