1943-79-9Relevant academic research and scientific papers
A very concise synthesis of a potent N-(1,3-thiazol-2-yl)pyridin-2-amine KDR kinase inhibitor
Zhao, Matthew,Yin, Jingjun,Huffman, Mark A.,McNamara, James M.
, p. 1110 - 1115 (2006)
A very concise synthesis of a potent KDR kinase inhibitor 1 is described. The synthesis features an exceedingly efficient one-pot preparation of the aminothiazole 6 followed by Pd-Xantphos catalyzed cross-coupling with chloropyridine aldehyde 11. Reductiv
1,2,4-TRIAZOLINOE CB1 INHIBITORS
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Page/Page column 45, (2021/09/11)
Disclosed are compounds according to Formula (I), and related pharmaceutical compositions. Also disclosed are therapeutic methods, e.g., of treating diseases such as diabetic kidney disease, diabetic nephropathy, obesity-related kidney disease, focal segmental glomerular sclerosis, IgA nephropathy, nephrotic syndrome, kidney fibrosis, Prader Willi syndrome, metabolic syndrome, gastrointestinal diseases, non-alcoholic liver disease, alcoholic liver disease, or non-alcoholic fatty liver disease, using the compounds of Formula (I).
Catalytic Decarboxylative C?N Formation to Generate Alkyl, Alkenyl, and Aryl Amines
Zhang, Yipin,Ge, Xia,Lu, Hongjian,Li, Guigen
supporting information, p. 1845 - 1852 (2020/12/01)
Transition-metal-catalyzed sp2 C?N bond formation is a reliable method for the synthesis of aryl amines. Catalytic sp3 C?N formation reactions have been reported occasionally, and methods that can realize both sp2 and sp3 C?N formation are relatively unexplored. Herein, we address this challenge with a method of catalytic decarboxylative C?N formation that proceeds through a cascade carboxylic acid activation, acyl azide formation, Curtius rearrangement and nucleophilic addition reaction. The reaction uses naturally abundant organic carboxylic acids as carbon sources, readily prepared azidoformates as the nitrogen sources, and 4-dimethylaminopyridine (DMAP) and Cu(OAc)2 as catalysts with as low as 0.1 mol % loading, providing protected alkyl, alkenyl and aryl amines in high yields with gaseous N2 and CO2 as the only byproducts. Examples are demonstrated of the late-stage functionalization of natural products and drug molecules, stereospecific synthesis of useful α-chiral alkyl amines, and rapid construction of different ureas and primary amines.
The synthesis of phenyl carbamates catalyzed by iron (II) bromide: An oxidative approach for cross-coupling of phenols with formamides
Adurthi, Suryakumari,Sudhakar, Chithaluri,Vala, Manoj Kumar,Vanam, Shekhar
, (2021/12/30)
The carbamate group is a key structural motif in many approved drugs and pro-drugs. There is increasing use of carbamates in the medicinal chemistry and agrochemical industry. We present, reagents and chemical methodologies for the synthesis of carbamates, and recent applications. The direct coupling of simple phenols with mono- and di-alkyl formamides provided the phenylcarbamate products.
Highly efficient synthesis of hiv nnrti doravirine
Gauthier, Donald R.,Sherry, Benjamin D.,Cao, Yang,Journet, Michel,Humphrey, Guy,Itoh, Tetsuji,Mangion, Ian,Tschaen, David M.
supporting information, p. 1353 - 1356 (2015/03/30)
The development of an efficient and robust process for the production of HIV NNRTI doravirine is described. The synthesis features a continuous aldol reaction as part of a de novo synthesis of the key pyridone fragment. Conditions for the continuous flow aldol reaction were derived using microbatch snapshots of the flow process.
PROCESS FOR MAKING REVERSE TRANSCRIPTASE INHIBITORS
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Page/Page column 12; 13, (2015/06/18)
The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase and HIV replication, and the treatment of human immunodeficiency virus infection in humans.
PROCESS FOR MAKING REVERSE TRANSCRIPTASE INHIBITORS
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Page/Page column 20, (2014/06/24)
The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse t
Ligand-assisted copper-catalyzed oxidative cross-coupling of simple phenols with formamides for the synthesis of carbamates
Reddy, Nagireddy Veera,Kumar, Gadde Sathish,Kumar, Pailla Santhosh,Kantam, M. Lakshmi,Reddy, Kallu Rajender
supporting information, p. 2133 - 2138 (2014/11/08)
An oxidative approach for the synthesis of phenyl carbamates has been achieved by ligand-assisted copper-catalyzed cross-dehydrogenative coupling (CDC) of phenols with formamides. The direct coupling of simple phenols with mono- and dialkyl formamides pro
MONOCYCLIC PYRIDINE DERIVATIVE
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Paragraph 0272; 0273; 0274, (2014/09/03)
The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein n represents 0 to 2; A represents an arylene group or a heteroarylene group; G represents a single bond, an oxygen atom or —CH2—; E represents a nitrogen-containing non-aromatic heterocycle; R1 represents an alkoxy group or the like; R2 represents a hydrogen atom or the like; and R3 represents a hydrogen atom, an alkyl group, an alkoxy group or the like, with the proviso that when E represents an azetidine ring and R2 or R3 is present on a nitrogen atom on the azetidine ring, the R2 or R3 does not represent a hydrogen atom.
CHEMICAL COMPOUNDS
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Page/Page column 132, (2009/03/07)
In one aspect, the present invention relates to compounds of Formula (I): to pharmaceutically acceptable sa lts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.
