- From Pyridine- N-oxides to 2-Functionalized Pyridines through Pyridyl Phosphonium Salts: An Umpolung Strategy
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The reactions of pyridine-N-oxides with Ph3P under the developed conditions provide an unprecedented route to (pyridine-2-yl)phosphonium salts. Upon activation with DABCO, these salts readily serve as functionalized 2-pyridyl nucleophile equivalents. This umpolung strategy allows for the selective C2 functionalization of the pyridine ring with electrophiles, avoiding the generation and use of unstable organometallic reagents. The protocol operates at ambient temperature and tolerates sensitive functional groups, enabling the synthesis of otherwise challenging compounds.
- Bugaenko, Dmitry I.,Yurovskaya, Marina A.,Karchava, Alexander V.
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supporting information
p. 6099 - 6104
(2021/08/03)
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- Reaction of Pyridine-N-Oxides with Tertiary sp2-N-Nucleophiles: An Efficient Synthesis of Precursors for N-(Pyrid-2-yl)-Substituted N-Heterocyclic Carbenes
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N-(Pyrid-2-yl)-substituted azolium and pyridinium salts, precursors for hybrid NHC-containing ligands, were obtained with excellent regioselectivity, employing a deoxygenative CH-functionalization of pyridine-N-oxides with substituted imidazoles, thiazoles, and pyridine. Unlike the traditional SNAr-based methods, this approach provides high yields for substrates bearing substituents of different electronic nature. The utility of azolium and pyridinium salts thus prepared was also highlighted by the synthesis of pyridyl-substituted imidazolyl-2-thione, benzodiazepine as well as 2-aminopyridines.
- Bugaenko, Dmitry I.,Karchava, Alexander V.,Yurovskaya, Marina A.
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supporting information
p. 5777 - 5782
(2020/12/01)
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- NRF2 REGULATORS
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Provided are aryl analogs,pharmaceutical compositions containing them and their use as NRF2 regulators.
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Page/Page column 452
(2017/01/02)
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- DOPAMINE D3 RECEPTOR ANTAGONISTS COMPOUNDS
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The disclosure is directed to novel dopamine D3 receptor antagonists, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, including treating drug dependency and psychosis.
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Page/Page column 124
(2016/05/19)
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- ALKYNYL ALCOHOLS AND METHODS OF USE
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The invention relates to compounds of Formula (0): wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.
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Paragraph 1232; 1233
(2015/03/04)
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- ALKYNYL ALCOHOLS AND METHODS OF USE
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The invention relates to compounds of Formula (0): wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.
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Page/Page column 268
(2015/03/13)
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- DIMETHYLBENZOIC ACID COMPOUNDS
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The present invention provides a compound of the Formula I: wherein A is: and W, Y, X, R1, R2, R3, and R4 are as defined herein, or a pharmaceutically acceptable salt thereof, for use as an inhibitor of the EP4 receptor.
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Page/Page column 11
(2015/07/07)
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- SUBSTITUTED BENZOFURAN COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. (I)
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Page/Page column 69
(2015/01/16)
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- SUBSTITUTED BENZOFURAN COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES
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Disclosed are compounds of formula (I) that are useful as hepatitis C virus (HCV) NSSB polymerise inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NSSB polymerise activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
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Page/Page column 72; 73
(2015/01/16)
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- Synthesis and SAR study of pyrrolo[3,4-b]pyridin-7(6H)-one derivatives as melanin concentrating hormone receptor 1 (MCH-R1) antagonists
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The discovery and optimization of novel pyrrolo[3,4-b]pyridin-7(6H)-one MCH-R1 antagonists are described. A systematic SAR study probing the effects of aryl-, benzyl- and arylthio-substituents at the 2-position of the pyrrolo[3,4-b]pyridin-7(6H)-ones led to identification of the 2-[(4-fluorophenyl)thio] derivative 7b as a highly potent MCH-R1 antagonist. This compound also has favorable pharmacokinetic properties along with a high metabolic stability and a minimal impact on CYP isoforms and hERG.
- Lim, Chae Jo,Kim, Ji Young,Lee, Byung Ho,Oh, Kwang-Seok,Yi, Kyu Yang
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supporting information
p. 1736 - 1739
(2013/04/10)
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- Synthesis of 5-amino or 4-amino substituted 7-AZA-isoindolin-1-ones
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A simple and convenient route for the synthesis of a series of 5-amino or 4-amino substituted 7-aza-isoindolin-1-ones is described. Amino substituted pyridine derivatives were cyclized with different amines in alkaline condition to give the desired produc
- Zhou, Heng,Shi, Qunfeng,Liu, Xiangchao,Zhan, Xiaoping,Liu, Zenglu,Mao, Zhenmin
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p. 1279 - 1287
(2013/07/05)
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- Synthesis of 4-methoxy and 5-methoxy substituted 7-aza-isoindolin-1-ones
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A simple and convenient route for the synthesis of a series of 4-methoxy or 5-methoxy substituted 7-aza-isoindolin-1-ones is described. Methoxyl substituted pyridine derivatives were cyclized with different amines under alkaline condition to give the desi
- Zhou, Heng,Sun, Guanglong,Liu, Zenglu,Zhan, Xiaoping,Mao, Zhenmin
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p. 2071 - 2079
(2013/10/22)
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- ADAMANTYL DERIVATES AS P2X7 RECEPTOR ANTAGONISTS
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The invention provides compounds of formula (I) pharmaceutically acceptable salt or solvate thereof, in which R1, A1, m and A are as defined in the specification; a process for their preparation; pharmaceutical compositions containin
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Page/Page column 152-153
(2010/10/20)
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