- Meta C-H Arylation of Electron-Rich Arenes: Reversing the Conventional Site Selectivity
-
Controlling site selectivity of C-H activation without using a directing group remains a significant challenge. While Pd(II) catalysts modulated by a mutually repulsive pyridine-type ligand have been shown to favor the relatively electron-rich carbon centers of arenes, reversing the selectivity to favor palladation at the relatively electron-deficient positions has not been possible. Herein we report the first catalytic system that effectively performs meta C-H arylation of a variety of alkoxy aromatics including 2,3-dihydrobenzofuran and chromane with exclusive meta site selectivity, thus reversing the conventional site selectivity governed by native electronic effects. The identification of an effective ligand and modified norbornene (NBE-CO2Me), as well as taking advantage of the statistics, are essential for achieving the exclusive meta selectivity.
- Liu, Luo-Yan,Qiao, Jennifer X.,Yeung, Kap-Sun,Ewing, William R.,Yu, Jin-Quan
-
supporting information
p. 14870 - 14877
(2019/10/02)
-
- CERTAIN CHEMICAL ENTITES, COMPOSITIONS, AND METHODS
-
Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.
- -
-
Paragraph 0185
(2013/04/10)
-
- CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
-
Chemical entities based on quinoxaline that are kinase inhibitors are described. Specifically quinoxaline derivatives of Formula I, containing a diarylamide or diarylurea substructure that inhibit Braf mutant kinase activity, pharmaceutical compositions c
- -
-
Paragraph 0196
(2013/03/28)
-
- Activity of novel quinoxaline-derived chalcones on in vitro glioma cell proliferation
-
Gliomas are the most common and devastating tumors of the central nervous system (CNS). Many pieces of evidence point out the relevance of natural compounds for cancer therapy and prevention, including chalcones. In the present study, eight synthetic quin
- Mielcke, Tania R.,Mascarello, Alessandra,Filippi-Chiela, Eduardo,Zanin, Rafael F.,Lenz, Guido,Leal, Paulo César,Chirardia, Louise D.,Yunes, Rosendo A.,Nunes, Ricardo J.,Battastini, Ana M.O.,Morrone, Fernanda B.,Campos, Maria M.
-
p. 255 - 264
(2012/03/26)
-
- AROYLQUINOLINE COMPOUNDS
-
A serious of nitro heterocyclic derivatives including a structure of formula (I) are provided. In formula (I), P, Q and R1 to R8 are defined in the specification. The derivatives disclosed in the present invention are characterized in inhibiting tubulin p
- -
-
Page/Page column 12
(2011/11/13)
-
- NOVEL CURCUMIN DERIVATIVE
-
The present invention provides a novel compound that is structurally similar to curcumin and has a suppressive effect on Aβ aggregation, a degradative effect on Aβ aggregates, an inhibitory effect on β-secretase, and a protective effect on neurons. The novel compound is a compound represented by the following general formula (Ia) or a salt thereof: wherein R1 represents a 4-hydroxy-3-methoxyphenyl group or the like, and R2 represents a 1H-indol-6-yl group or the like.
- -
-
Page/Page column 66
(2009/12/07)
-
- Palladium/di-1-adamantyl-n-butylphosphine-catalyzed reductive carbonylation of aryl and vinyl halides
-
A general and efficient palladium-catalyzed reductive carbonylation with low catalyst loadings (0.5 mol % Pd or below) has been developed. The formylation of aryl and heteroaryl bromides proceeds smoothly in the presence of palladium/di-1-adamantyl-n-butylphosphine at ambient pressure of synthesis gas to afford the corresponding aromatic aldehydes in good yields and excellent selectivity. In addition, vinyl halides react under similar conditions to form α,β-unsaturated aldehydes in good yield.
- Brennführer, Anne,Neumann, Helfried,Klaus, Stefan,Riermeier, Thomas,Almena, Juan,Beller, Matthias
-
p. 6252 - 6258
(2008/02/04)
-
- Piperazinylimidazopyridine and piperazinyltriazolopyridine antagonists of gonadotropin releasing hormone receptor
-
The present invention relates to Gonadotropin Releasing Hormone (GnRH, also known as Luteinizing Hormone Releasing Hormone) receptor antagonists.
- -
-
Page/Page column 37
(2008/06/13)
-
- NOVEL CHEMICAL COMPOUNDS
-
This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with hYAK3 activity.
- -
-
-
- (5Z)-5-(6-QUINOXALINYLMETHYLIDENE)-2-[(2,4,6-TRICHLOROPHENYL)AMINO]-1,3-THIAZOL-4(5H)-ONE
-
Invented is the compound (5Z)-5-(6-quinoxalinylmethylidene)-2-[(2,4,6-trichlorophenyl)amino]-1 ,3-thiazol-4(5H)-one, and pharmaceutically acceptable salts, hydrates, solvates and pro-drugs thereof. Also invented are pharmaceutical compositions containg this compound, methods of preparing this compound and pharmaceutically acceptable salts, hydrates, solvates and pro-drugs thereof. Also invented are methods of using this compound as an inhibitor of hYAK3 proteins.
- -
-
Page/Page column 7
(2008/06/13)
-
- PYRIMIDINYLPYRAZOLES AS TGF-BETA INHIBITORS
-
The invention is based on the discovery that compounds of formula (I) possess high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders. The invention feat
- -
-
Page/Page column 33
(2010/10/20)
-
- A new family of quinoline and quinoxaline analogues of combretastatins
-
The 3-hydroxy-4-methoxyphenyl ring of combretastatin A-4 can be replaced by a 2-naphthyl moiety without significant loss of cytotoxicity and inhibition of tubulin polymerization potency. In this paper we show that the 6- or 7-quinolyl systems can in turn replace both cyclic moieties, keeping in the first case most of the potency as cytotoxic agent and in the second case as inhibitor of tubulin polymerization, related to the activities displayed by model compounds.
- Perez-Melero, Concepcion,Maya, Ana B.S.,Del Rey, Benedicto,Pelaez, Rafael,Caballero, Esther,Medarde, Manuel
-
p. 3771 - 3774
(2007/10/03)
-
- AZOLIDINONE-VINYL FUSED-BENZENE DERIVATIVES
-
The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, graft rejection or lung injuries. Formula (I), wherein A, X, Y, Z, R1 , R2 and n are as described in the description.
- -
-
-
- Method for preparing heterocyclic-carboxylic acids
-
The present invention relates to a method for preparing quinoxaline-5- and 6-carboxylic acids. The method comprises contacting an aqueous suspension of a 5- or 6-hydroxymethyl quinoxaline with oxygen in the presence of a transition metal catalyst, to form the respective quinoxaline-5- or 6-carboxylic acid. The method for oxidizing benzylic methyl groups may also be employed to prepare a wide variety of heterocyclic carboxylic acid compounds.
- -
-
-
- (1H-azol-1-ylmethyl)substituted quinoxaline derivatives
-
(1H-azol-1-ylmethyl)substituted quinoxaline derivatives, compositions containing the same, and methods of treating mammals suffering from disorders which are characterized by an increased proliferation and/or abnormal differentiation of epithelial tissues
- -
-
-