cas 209412-06-6, 2-(6-CHLORO-3-PYRIDAZINYL)-2-(2,6-DICHLOROPHENYL)ACETONITRILE

Articles about 209412-06-6Total 5 be found

Rapid synthesis of VX-745: p38 MAP kinase inhibition in Werner syndrome cells
The p38 mitogen-activated protein kinase inhibitor VX-745 is prepared rapidly and efficiently in a four-step sequence using a combination of conductive heating and microwave-mediated steps. Its inhibitory activity was confirmed in hTERT immortalized HCA2
Bagley, Mark C.,Davis, Terence,Dix, Matthew C.,Rokicki, Michal J.,Kipling, David
p. 5107 - 5110
(2007)
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NITROGEN-CONTAINING HETEROCYCLIC COMPOUND AND COMPOSITION THEREOF, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF
Disclosed by the present invention are a nitrogen-containing heterocyclic compound, and a composition thereof, a preparation method therefor and an application thereof. The structure of the nitrogen-containing heterocyclic compound according to the presen
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Paragraph 0183-0184

(2021/10/07)

The discovery of VX-745: A novel and selective p38α kinase inhibitor
The synthesis of novel, selective, orally active 2,5-disubstituted 6H-pyrimido[1,6-b]pyridazin-6-one p38α inhibitors is described. Application of structural information from enzyme-ligand complexes guided the selection of screening compounds, leading to t
Duffy, John P.,Harrington, Edmund M.,Salituro, Francesco G.,Cochran, John E.,Green, Jeremy,Gao, Huai,Bemis, Guy W.,Evindar, Ghotas,Galullo, Vincent P.,Ford, Pamella J.,Germann, Ursula A.,Wilson, Keith P.,Bellon, Steven F.,Chen, Guanging,Taslimi, Paul,Jones, Peter,Huang, Cassey,Pazhanisamy,Wang, Yow-Ming,Murcko, Mark A.,Su, Michael S.S.
supporting information; experimental part
p. 758 - 763
(2011/12/03)

Microwave-assisted Ullmann C-S bond formation: Synthesis of the P38α MAPK clinical candidate VX-745
(Chemical Equation Presented) Microwave irradiation promotes the rapid and efficient reaction of a thiophenol and aryl or heteroaryl halide using a copper or palladium catalyst and a range of ligands, depending upon substrate. Of particular utility is the use of copper(I) iodide (5 mol %) and trans-cyclohexane-1,2-diol as ligand under basic conditions and microwave irradiation to give the corresponding sulfide in high yield. This method for C-S bond formation is applied in the four-step synthesis of the clinical candidate VX-745 in 38% overall yield. The inhibitory activity of VX-745 against p38α MAPK is confirmed in Werner syndrome dermal fibroblasts at 1.0 μM concentration by immunoblot assay. 2009 American Chemical Society.
Bagley, Mark C.,Davis, Terence,Dix, Matthew C.,Fusillo, Vincenzo,Pigeaux, Morgane,Rokicki, Michal J.,Kipling, David
experimental part
p. 8336 - 8342
(2010/03/01)

An improved synthesis of 5-(2,6-dichlorophenyl)-2-(phenylthio)-6H- pyrimido[1,6-b]pyridazin-6-one (a VX-745 analog)
An improved procedure for the synthesis an analog of the p38 inhibitor compound VX-745 is reported.
Treu, Matthias,Jordis, Ulrich,Lee, Ving J.
p. 959 - 963
(2007/10/03)