71146-13-9Relevant academic research and scientific papers
Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion
Konteatis, Zenon,Travins, Jeremy,Gross, Stefan,Marjon, Katya,Barnett, Amelia,Mandley, Everton,Nicolay, Brandon,Nagaraja, Raj,Chen, Yue,Sun, Yabo,Liu, Zhixiao,Yu, Jie,Ye, Zhixiong,Jiang, Fan,Wei, Wentao,Fang, Cheng,Gao, Yi,Kalev, Peter,Hyer, Marc L.,Delabarre, Byron,Jin, Lei,Padyana, Anil K.,Dang, Lenny,Murtie, Joshua,Biller, Scott A.,Sui, Zhihua,Marks, Kevin M.
supporting information, p. 4430 - 4449 (2021/05/06)
The metabolic enzyme methionine adenosyltransferase 2A (MAT2A) was recently implicated as a synthetic lethal target in cancers with deletion of the methylthioadenosine phosphorylase (MTAP) gene, which is adjacent to the CDKN2A tumor suppressor and codelet
INHIBITORS OF CELLULAR METABOLIC PROCESSES
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Page/Page column 49-50, (2018/03/25)
The invention provides inhibitor compounds of MAT2A that are useful as therapeutic agents for treating malignancies wherein the compounds have the general formula (I) : wherein ring A, ring B, ring C and, R1 are as described herein.
Thermolysis of 2-diazo-3-aryl ketoesters: New route to α-aryl malonates and aromatic esters
Zhang, Zhao,Tang, Mengyao,Zang, Lei,Zou, Liang-Hua,Li, Jie
supporting information, p. 5681 - 5684 (2016/11/28)
Thermochemical excitation enabled efficient α-aryl malonates synthesis from 2-diazo-3-aryl ketoesters and alcohols under transition metal-free reaction conditions. Furthermore, an unusual C[sbnd]C bond cleavage and C[sbnd]O/(N) bond formation occurred whe
γ-methylidene-δ-valerolactones as a coupling partner for cycloaddition: Palladium-catalyzed [4 + 3] cycloaddition with nitrones
Shintani, Ryo,Murakami, Masataka,Hayashi, Tamio
, p. 12356 - 12357 (2008/03/27)
A new type of reagent, γ-methylidene-δ-valerolactones, has been devised, which acts as a four-carbon unit in a palladium-catalyzed cycloaddition reaction through the formation of a 1,4-zwitterionic species. The utility has been demonstrated in the context of stereoselective [4 + 3] cycloaddition with nitrones to provide highly functionalized 1,2-oxazepines, including the asymmetric variant with high enantioselectivity. Copyright
Copper-catalyzed formation of carbon-heteroatom and carbon-carbon bonds
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, (2015/03/06)
The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-oxygen bond between the oxygen atom of an alcohol and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. The present invention also relates to copper-catalyzed methods of forming a carbon-carbon bond between a reactant comprising a nucleophilic carbon atom, e.g., an enolate or malonate anion, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. Importantly, all the methods of the present invention are relatively inexpensive to practice due to the low cost of the copper comprised by the catalysts.
Anti-mycobacterial 4-hydroxy-3-phenylpyridin-2(1H)-ones
Dannhardt, G,Meindl, W,Schober, B D,Kappe, T
, p. 599 - 604 (2007/10/02)
4-Hydroxy-3-phenylpyridin-2 (1H)-ones with different substituents either at N-1 or in the phenyl group were synthesized by reaction of ethyl β-aminocrotonates with dialkyl malonates or 'magic malonates' (2,4,6-trichlorophenyl malonates).The evaluation of these compounds on Mycobacterium tuberculosis H37Ra, Escherichia coli B and Staphylococcus aureus ATCC 25923 showed significant inhibitory effects on M tuberculosis (5g and 5s, MIC=8μg/ml).A structure-activity relationship is discussed.
DIMETHYL ARYLMALONATES FROM CERIUM(IV) AMMONIUM NITRATE PROMOTED REACTIONS OF DIMETHYL MALONATE WITH AROMATIC COMPOUNDS IN METHANOL
Baciocchi, Enrico,Dell'Aira, Donatella,Ruzziconi, Renzo
, p. 2763 - 2766 (2007/10/02)
Aromatic compounds undergo homolytic malonylation by reaction with cerium(IV) ammonium nitrate and dimethyl malonate in methanol at room temperature.
