202409-85-6Relevant academic research and scientific papers
Preparation technology of etoricoxib and reference substance 5-chloro-3-(4-(methyl sulphonyl)phenyl)-2,3-bipyridine of etoricoxib
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, (2017/08/28)
The invention discloses a preparation technology of etoricoxib and a reference substance 5-chloro-3-(4-(methyl sulphonyl)phenyl)-2,3-bipyridine of etoricoxib. The preparation technology comprises steps as follows: 5-chloro-2-hydroxypyridine is taken as a raw material and subjected to a substitution reaction, and 5-chloro-3-iodopyridine-2-ol is obtained; 5-chloro-3-iodopyridine-2-ol is subjected to a coupled reaction, and 5-chloro-3-(4-(methyl sulphonyl)phenyl)pyridine-2-ol is obtained; 5-chloro-3-(4-(methyl sulphonyl)phenyl)pyridine-2-ol is subjected to the substitution reaction, and 2-bromo-5-chloro-3-(4-(methyl sulphonyl)phenyl)pyridine is obtained; 2-bromo-5-chloro-3-(4-(methyl sulphonyl)phenyl)pyridine is subjected to the coupled reaction, a target product etoricoxib or the reference substance 5-chloro-3-(4-(methyl sulphonyl)phenyl)-2,3-bipyridine of etoricoxib is obtained, and the total yield can reach 18%. The route is one novel technology for synthesizing etoricoxib or the reference substance 5-chloro-3-(4-(methyl sulphonyl)phenyl)-2,3-bipyridine of etoricoxib, and the blank of a synthesis method of the reference substance 5-chloro-3-(4-(methyl sulphonyl)phenyl)-2,3-bipyridine of etoricoxib in China is filled up accordingly.
A facile synthesis of 3,5-halo and aryl 1H-pyridin-2-ones from pyridinium N-(pyridin-2-yl)aminide
Filace, Fabiana,Sucunza, David,Izquierdo, M. Luisa,Burgos, Carolina,Alvarez-Builla, Julio
, p. 6088 - 6094 (2013/07/19)
The synthesis of halogenated and arylated 1H-pyridin-2-ones starting from pyridinium N-(pyridin-2-yl)aminides is described. The synthetic pathway involves the reaction of pyridinium N-(5-bromopyridin-2-yl)aminide, N-(3-bromo-5- chloropyridin-2-yl)aminide or N-(3,5-dibromopyridin-2-yl)aminide with different boronic acids to afford monosubstituted and disubstituted aminides in good yields. An additional bromination in the 3-position of N-(5-arylpyridin-2-yl) aminides was performed. Finally, reduction of the N-N bond followed by the reaction of the corresponding 2-aminopyridines with sodium nitrite/sulfuric acid in water yields 3,5-disubstituted 1H-pyridin-2-ones in good yields.
Phosphorodiamidate-directed metalation of N -heterocycles using Mg- and Zn-TMP bases
Rohbogner, Christoph J.,Wirth, Stefan,Knochel, Paul
supporting information; experimental part, p. 1984 - 1987 (2010/07/15)
Figure presented The strong directing ability of the N,N,N′,N′- tetramethyldiaminophosphorodiamidate group has been used to achieve selective metalations on various heterocycles such as pyridines, quinolines and quinoxalines with TMP-derived bases like TMPMgCl·LiCl, TMP 2Mg·2LiCl, and TMP2Zn·2MgCl 2·2LiCl. This protocol was applied in the synthesis of etoricoxib, talnetant and a P-selectin inhibitor.
Combination therapy for reducing the risks associated with cardio-and-cerebrovascular disease
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, (2008/06/13)
The instant invention provides a drug combination comprised of an HMG-CoA reductase inhibitor in combination with a COX-2 inhibitor, which is useful for treating, preventing, and/or reducing the risk of developing atherosclerosis and atherosclerotic disease events.
Substituted pyridines as selective cyclooxygenase-2 inhibitors
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, (2008/06/13)
The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. STR1 The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.
